标签归档：leu

(R)-MG-132(Synonyms: (S,R,S)-(-)-MG-132 Z-Leu-D-Leu-Leu-al)

发表于由

(R)-MG-132;(Synonyms: (S,R,S)-(-)-MG-132; Z-Leu-D-Leu-Leu-al) 纯度: ge;98.0%

(R)-MG-132 ((S,R,S)-(-)-MG-132) 是 MG-132 的一种对映异构体。(R)-MG-132 是蛋白酶体 (proteasome) 抑制剂。(R)-MG-132 细胞毒性比 MG-132 弱。(R)-MG-132 是比 MG-132 更有效的 proteasome 抑制剂。

(R)-MG-132amp;;(Synonyms: (S,R,S)-(-)-MG-132; Z-Leu-D-Leu-Leu-al)

(R)-MG-132 Chemical Structure

CAS No. : 1211877-36-9

规格 价格 是否有货 数量
5 mg ￥800 In-stock
10 mg ￥1200 In-stock
50 mg ￥4200 In-stock
100 mg ￥6800 In-stock
200 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

(R)-MG-132 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

(R)-MG-132 ((S,R,S)-(-)-MG-132) is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132. (R)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132[1].

IC50 Target

Proteasome[1]
体外研究
(In Vitro)

(R)-MG-132, the stereoisomer of MG-132, is studied as a potential inhibitor of chymotrypsin-like, trypsin-like, and peptidylglutamyl peptide hydrolyzing activities of proteasome[1].
MG-132 and (R)-MG-132 are investigated for inhibition of ChTL, trypsin-like (TL) and peptidylglutamyl peptide hydrolyzing (PGPH) activities of purified 20S proteasomes isolated from human erythrocytes. For MG-132, the IC50s of 0.89 μM, 104.43 μM, and 5.7 μM for ChTL, TL, and PGPH, respectively. For (R)-MG-132, the IC50s of 0.22 μM, 34.4 μM, and 2.95 μM for ChTL, TL, and PGPH, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

475.62

Formula

C26H41N3O5
CAS 号

1211877-36-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : 100 mg/mL (210.25 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1025 mL 10.5126 mL 21.0252 mL
5 mM 0.4205 mL 2.1025 mL 4.2050 mL
10 mM 0.2103 mL 1.0513 mL 2.1025 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.26 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (5.26 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 0.83 mg/mL (1.75 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (1.75 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Mroczkiewicz M, et al. Studies of the synthesis of all stereoisomers of MG-132 proteasome inhibitors in the tumor targeting approach. J Med Chem. 2010 Feb 25;53(4):1509-18.

N-Boc-Phe-Leu-Phe-Leu-Phe(Synonyms: Boc-FLFLF)

发表于由

N-Boc-Phe-Leu-Phe-Leu-Phe;(Synonyms: Boc-FLFLF) 纯度: 98.33%

N-Boc-Phe-Leu-Phe-Leu-Phe (Boc-FLFLF) 是一种甲酰肽受体 1 (FPR1) 拮抗剂，可增加疼痛作用并抑制膜联蛋白的抗疼痛活性。

N-Boc-Phe-Leu-Phe-Leu-Pheamp;;(Synonyms: Boc-FLFLF)

N-Boc-Phe-Leu-Phe-Leu-Phe Chemical Structure

CAS No. : 148182-34-7

规格 价格 是否有货 数量
1 mg ￥900 In-stock
5 mg ￥2000 In-stock
10 mg ￥3600 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

N-Boc-Phe-Leu-Phe-Leu-Phe 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

N-Boc-Phe-Leu-Phe-Leu-Phe (Boc-FLFLF) is a formyl peptide receptor 1 (FPR1) antagonist, which increases pain effects and inhibits antinociceptive activity of annexin[1][2].

IC50 Target

FPR1[1]
分子量

785.97

Formula

C44H59N5O8
CAS 号

148182-34-7
Sequence Shortening

Boc-FLFLF
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : 100 mg/mL (127.23 mM; Need ultrasonic)

H2O : 1 mg/mL (1.27 mM; ultrasonic and warming and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2723 mL 6.3616 mL 12.7231 mL
5 mM 0.2545 mL 1.2723 mL 2.5446 mL
10 mM 0.1272 mL 0.6362 mL 1.2723 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.18 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Schepetkin IA, et al. Antagonism of human formyl peptide receptor 1 (FPR1) by chromones and related isoflavones. Biochem Pharmacol. 2014 Dec 15;92(4):627-41.

    [2]. Pei L, et al. Annexin 1 exerts anti-nociceptive effects after peripheral inflammatory pain through formyl-peptide-receptor-like 1 in rat dorsal root ganglion. Br J Anaesth. 2011 Dec;107(6):948-58.

N-Formyl-Met-Leu-Phe(Synonyms: fMLP N-Formyl-MLF)

发表于由

N-Formyl-Met-Leu-Phe;(Synonyms: fMLP; N-Formyl-MLF) 纯度: 99.81%

N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) 是一种趋化肽和N-甲酰基肽受体 (FPR) 的特异性配体。报道显示N-Formyl-Met-Leu-Ph 可抑制 TNF-alpha 的分泌。

N-Formyl-Met-Leu-Pheamp;;(Synonyms: fMLP; N-Formyl-MLF)

N-Formyl-Met-Leu-Phe Chemical Structure

CAS No. : 59880-97-6

规格 价格 是否有货 数量
5 mg ￥500 In-stock
10 mg ￥900 In-stock
50 mg ￥1900 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

* Please select Quantity before adding items.

N-Formyl-Met-Leu-Phe 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptidomimetic Library
  • Peptide Library

生物活性

N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) is a chemotactic peptide and a specific ligand of N-formyl peptide receptor (FPR). N-Formyl-Met-Leu-Ph is reported to inhibit TNF-alpha secretion.

IC50 Target

TNF-alpha[1]
体外研究
(In Vitro)

Binding of N-Formyl-Met-Leu-Phe to its specific cell surface receptor, N-formyl peptide receptor (FPR), triggers different cascades of biochemical events, eventually leading to cellular activation. FPR is a chemoattractant receptor belonging to the G protein-coupled receptor family. N-Formyl-Met-Leu-Phe promotes osteoblastic commitment and suppresses adipogenic commitment under osteoblastic differentiation conditions. N-Formyl-Met-Leu-Phe stimulates osteogenesis is associated with increased expression of osteogenic markers and mineralization. N-Formyl-Met-Leu-Phe inhibits expression of peroxisome proliferator-activated receptor-γ1. N-Formyl-Met-Leu-Phe-stimulated osteogenic differentiation is mediated via FPR1-phospholipase C/phospholipase D-Ca2+-calmodulin-dependent kinase II-ERK-CREB signaling pathways[1]. N-Formyl-Met-Leu-Phe, a bacterial-derived peptide, induced proinflammatory cytokine gene expression in human peripheral blood monocytes. Bacterial products LPS and N-Formyl-Met-Leu-Phe synergistically induce inflammatory response via multiple signaling pathways. TLR4, IKKβ-IκBα, and NF-κB signaling pathways are involved in the synergistic induction of TNF-α via p65 nuclear translocation-dependent mechanisms[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

N-Formyl-Met-Leu-Phe promotes bone formation in zebrafish and rabbits. Extensive skeletal development is evident at 5 dpf in over 80% of N-Formyl-Met-Leu-Phe-treated zebrafish. Treatment with N-Formyl-Met-Leu-Phe results in increased expression of Runx2. Bone marrow spaces are widely formed, and connective tissue covering bone is dense, like periosteum, in N-Formyl-Met-Leu-Phe-treated calvaria[1]. N-Formyl-Met-Leu-Phe mediate release of calprotectin from PMN in vitro. It induces release of calprotectin from PMN in a dose dependent manner. A minimum of 10% of total PMN calprotectin is retained at concentrations of 0.1-10.0 nM of N-Formyl-Met-Leu-Phe[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

437.55

Formula

C21H31N3O5S
CAS 号

59880-97-6
Sequence

Formyl-Met-Leu-Phe
Sequence Shortening

Formyl-MLF
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : ≥ 82.5 mg/mL (188.55 mM)

H2O : < 0.1 mg/mL (ultrasonic) (insoluble)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2855 mL 11.4273 mL 22.8545 mL
5 mM 0.4571 mL 2.2855 mL 4.5709 mL
10 mM 0.2285 mL 1.1427 mL 2.2855 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.75 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.75 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Shin MK, et al. N-formyl-methionyl-leucyl-phenylalanine (fMLP) promotes osteoblast differentiation via the N-formyl peptide receptor 1-mediated signaling pathway in human mesenchymal stem cells from bone marrow. J Biol Chem. 2011 May 13;286(19):17133-43.

    [2]. Chen LY, et al. Synergistic induction of inflammation by bacterial products lipopolysaccharide and fMLP: an important microbial pathogenic mechanism. J Immunol. 2009 Feb 15;182(4):2518-24.

    [3]. Hetland G, et al. Chemotaxins C5a and fMLP induce release of calprotectin (leucocyte L1 protein) from polymorphonuclear cells in vitro. Mol Pathol. 1998 Jun;51(3):143-8.
Cell Assay
[2]

Cells are cotransfected with either a dominant negative form of IκBα or a dominant negative form of IKKβ together with the NF-κB-dependent luciferase reporter plasmid. The plasmid pCMVβ is used as a control for transfection efficiency and this is monitored via the expression of β-galactosidase. Cells are transiently transfected with plasmids using DEAE-dextran. The transfected cells are cultivated for 48 h before a 6-h incubation in medium ±N-Formyl-Met-Leu-Phe, LPS, or N-Formyl-Met-Leu-Phe/LPS. Luciferase activity is determined by using the luciferase assay kit and a Monolight 3010 luminometer[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: N-Formyl-Met-Leu-Phe is prepared in sterile PBS. Under the anesthesia, mice are intranasally treated with LPS (0.3 mg/kg) or N-Formyl-Met-Leu-Phe (0.5 mg/kg) or N-Formyl-Met-Leu-Phe and LPS in 50 μL of sterile PBS (control), BAL is performed by cannulating the trachea with sterilized PBS, and cells from BAL fluid are stained with Wright-Giemsa stain after cytocentrifuge. For TNF-α protein release, BAL fluid is collected and secreted TNF-α is measured by ELISA as described above[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Shin MK, et al. N-formyl-methionyl-leucyl-phenylalanine (fMLP) promotes osteoblast differentiation via the N-formyl peptide receptor 1-mediated signaling pathway in human mesenchymal stem cells from bone marrow. J Biol Chem. 2011 May 13;286(19):17133-43.

    [2]. Chen LY, et al. Synergistic induction of inflammation by bacterial products lipopolysaccharide and fMLP: an important microbial pathogenic mechanism. J Immunol. 2009 Feb 15;182(4):2518-24.

    [3]. Hetland G, et al. Chemotaxins C5a and fMLP induce release of calprotectin (leucocyte L1 protein) from polymorphonuclear cells in vitro. Mol Pathol. 1998 Jun;51(3):143-8.

Boc-Leu-Gly-Arg-AMC

发表于由

Boc-Leu-Gly-Arg-AMC; 纯度: 99.64%

Boc-Leu-Gly-Arg-AMC 是一种转化酶的荧光 AMC 底物，可用于酶促测定。

Boc-Leu-Gly-Arg-AMCamp;;

Boc-Leu-Gly-Arg-AMC Chemical Structure

CAS No. : 65147-09-3

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ￥2150 In-stock
10 mg ￥1950 In-stock
50 mg ￥6600 In-stock
100 mg ￥11500 In-stock
200 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

Boc-Leu-Gly-Arg-AMC 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Endocrinology Compound Library
  • Peptide Library

生物活性

Boc-Leu-Gly-Arg-AMC is a fluorogenic AMC substrate for the convertases. Boc-Leu-Gly-Arg-AMC can be used in enzymatic assays[1][2].

体外研究
(In Vitro)

To demonstrate the presence in the abdominal gland of proteolytic enzymes capable of generating Sodefrin, an enzymatic assay was developed using Boc-Leu-Gly-Arg-AMC as synthetic substrate. A crude extract of the abdominal gland hydrolyzed Boc-Leu-Gly-Arg-AMC to liberate 7-amino-4- methylcoumarin, suggesting that enzymes that generate sodefrin from its precursor molecule are present in the gland. The activity in the extract for cleaving Boc-Leu-Gly-Arg-AMC is optimal at pH 9.0 and 45 ℃[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

601.69

Formula

C29H43N7O7
CAS 号

65147-09-3
Sequence

Boc-Leu-Gly-Arg-AMC
Sequence Shortening

Boc-LGR-AMC
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture and light

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:;

DMSO : 100 mg/mL (166.20 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6620 mL 8.3099 mL 16.6199 mL
5 mM 0.3324 mL 1.6620 mL 3.3240 mL
10 mM 0.1662 mL 0.8310 mL 1.6620 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.15 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.15 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Nakada T, et al. Evidence for processing enzymes in the abdominal gland of the newt, Cynops pyrrhogaster, that generate sodefrin from its biosynthetic precursor. Zoolog Sci. 2007 May;24(5):521-4.

    [2]. Yumiko Obayashi, et al. Proteolytic enzymes in coastal surface seawater: Significant activity of endopeptidases and exopeptidases Limnol. Oceanogr., 50(2), 2005, 722-726.

[Leu5]-Enkephalin(Synonyms: Leu-enkephalin Leucine enkephalin Leucyl-enkephalin)

发表于由

[Leu5]-Enkephalin;(Synonyms: Leu-enkephalin; Leucine enkephalin; Leucyl-enkephalin) 纯度: 99.81%

[Leu5]-Enkephalin 是一种具有吗啡药性的五肽。作为阿片受体 (opioid receptors) 激动剂。

[Leu5]-Enkephalinamp;;(Synonyms: Leu-enkephalin; Leucine enkephalin; Leucyl-enkephalin)

[Leu5]-Enkephalin Chemical Structure

CAS No. : 58822-25-6

规格 价格 是否有货 数量
10;mM;*;1 mL in Water ￥605 In-stock
10 mg ￥550 In-stock
25 mg ￥1100 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

[Leu5]-Enkephalin 相关产品

bull;相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Metabolism/Protease Compound Library
  • Neuronal Signaling Compound Library
  • Natural Product Library
  • Human Endogenous Metabolite Compound Library
  • Peptidomimetic Library
  • Phenols Library
  • Neurotransmitter Receptor Compound Library

生物活性

[Leu5]-Enkephalin is a pentapeptide with morphine like properties. [Leu5]-Enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.

IC50 Target

Human Endogenous Metabolite

;

体外研究
(In Vitro)

Enkephalins (met- , leu-enkephalin, and enkephalin 8) and dynorphins are two classes of opioid peptides found in the spinal dorsal horn. Mu, delta, and kappa are three major subtypes of opioid receptors. Enkephalins are putative endogenous ligands for delta opioid receptors, and dynorphins are endogenous ligands for the kappa opioid receptors. Three receptor types resembling the vertebrate δ- and κ-type opioid receptors have been characterized pharmacologically in nervous tissues (e.g. Ki=18.9 nM for Leu-enkephalin) and localized by autoradiography at CHH terminals in the SG of C. maenas[1].Leucine-enkephalin is a pentapeptides with morphine like properties, naturally present in mammalian brain[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

555.62

Formula

C28H37N5O7
CAS 号

58822-25-6
Sequence

Tyr-Gly-Gly-Phe-Leu
Sequence Shortening

YGGFL
中文名称

[Leu5]-脑啡肽
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : ≥ 150 mg/mL (269.97 mM)

H2O : 100 mg/mL (179.98 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7998 mL 8.9990 mL 17.9979 mL
5 mM 0.3600 mL 1.7998 mL 3.5996 mL
10 mM 0.1800 mL 0.8999 mL 1.7998 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Leu-enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.

    [2]. Meunier JC, et al. Binding of Leu5-enkephalin and Met5-enkephalin to a particulate fraction from rat cerebrum. FEBS Lett. 1977 May 15;77(2):209-13.

Suc-Leu-Leu-Val-Tyr-AMC

发表于由

Suc-Leu-Leu-Val-Tyr-AMC; 纯度: 98.87%

Suc-Leu-Leu-Val-Tyr-AMC 是一种荧光底物。

Suc-Leu-Leu-Val-Tyr-AMCamp;;

Suc-Leu-Leu-Val-Tyr-AMC Chemical Structure

CAS No. : 94367-21-2

规格 价格 是否有货 数量
1 mg ￥660 In-stock
5 mg ￥1300 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

Suc-Leu-Leu-Val-Tyr-AMC 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Suc-Leu-Leu-Val-Tyr-AMC is a fluorogenic substrate.

体外研究
(In Vitro)

Suc-Leu-Leu-Val-Tyr-AMC (Suc-LLVY) is a membrane-permeable calpain-specific fluorogenic substrate, pteolytic hydrolysis of the peptidyl-7-amino bond liberates the highly fluorescent 7-amino-4-methylcoumarin (AMC) moiety[1]. The effect of TGF-β on hydrolysis of these substrates (e.g Suc-Leu-Leu-Val-Tyr-AMC) are assessed. Biliary epithelial H69 cells are incubated with 10, 1, 0.1, or 0 ng/mL TGF-β for 24 h. Substrate hydrolysis is then fluorometrically assessed in cytosolic extracts. Basal activity is 1.12, 8.33, and 14.52 nmol AMC/mg protein/min for suc-LLVY-AMC, z-LLE-AMC, and z-LLL-AMC hydrolysis, respectively[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

763.88

Formula

C40H53N5O10
CAS 号

94367-21-2
Sequence

Suc-Leu-Leu-Val-Tyr
Sequence Shortening

Suc-LLVY
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Protect from light, stored under nitrogen

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:;

DMSO : ≥ 20 mg/mL (26.18 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3091 mL 6.5455 mL 13.0911 mL
5 mM 0.2618 mL 1.3091 mL 2.6182 mL
10 mM 0.1309 mL 0.6546 mL 1.3091 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Roberta L. Debiasi, et al. Reovirus-Induced Apoptosis Is Preceded by Increased Cellular Calpain Activity and Is Blocked by Calpain Inhibitors. J Virol. 1999 Jan; 73(1): 695–701.

    [2]. Tadlock L, et al. Transforming growth factor-beta inhibition of proteasomal activity: a potential mechanism of growth arrest. Am J Physiol Cell Physiol. 2003 Aug;285(2):C277-85. Epub 2003 Mar 19.

    [3]. Gardner RC, et al. Characterization of peptidyl boronic acid inhibitors of mammalian 20 S and 26 S proteasomes and their inhibition of proteasomes in cultured cells. Biochem J. 2000 Mar, 2:447-54.
Kinase Assay
[3]

Immunoprecipitation is carried out for the two sets of samples, using the same amount of protein. The 20 S and 26 S proteasome immunoprecipitates are washed with 50 mM Hepes/KOH (pH 7.5), and 50 mM Hepes/KOH (pH 7.5) containing 2 mMATP, respectively, prior to the determination of peptidase activity using 50 μM suc-Leu- Leu-Val-Tyr-AMC as substrate in these buffers[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Roberta L. Debiasi, et al. Reovirus-Induced Apoptosis Is Preceded by Increased Cellular Calpain Activity and Is Blocked by Calpain Inhibitors. J Virol. 1999 Jan; 73(1): 695–701.

    [2]. Tadlock L, et al. Transforming growth factor-beta inhibition of proteasomal activity: a potential mechanism of growth arrest. Am J Physiol Cell Physiol. 2003 Aug;285(2):C277-85. Epub 2003 Mar 19.

    [3]. Gardner RC, et al. Characterization of peptidyl boronic acid inhibitors of mammalian 20 S and 26 S proteasomes and their inhibition of proteasomes in cultured cells. Biochem J. 2000 Mar, 2:447-54.

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA

发表于由

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA; 纯度: 99.38%

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA 是一种特定的神经肽 Y Y1 受体激动剂。[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA 也激活 Y4，Y5。[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA 可以增加麻醉大鼠的血压，也增加饮食摄入量。

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFAamp;;

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ￥4000 In-stock
10 mg ￥6800 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA slao activates Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA can increase blood pressure in anesthetized rats and increases food intake[1][2].

IC50 Target[1][2]

NPY Y1 receptor

;

NPY Y4 receptor

;

NPY Y5 receptor

;

体外研究
(In Vitro)

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA has Ki values of 0.39 nM, 0.499 nM, 0.31 nM for Y1, Y4, Y5 in HEK cell lines. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA has a Ki of >1000 for Y2 in HEK cell lines[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA (30 pmol; microinjected into paraventricular nucleus) increases food intake in the rats (350±400 g)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

4354.76

Formula

C191H285F3N54O58S
Sequence

Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala-Pro-Ala-Glu-Asp-Met-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-Leu-Thr-Arg-Pro-Arg-Tyr-NH2
Sequence Shortening

YPSKPDNPGEDAPAEDMARYYSALRHYINLLTRPRY-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:;

H2O : 50 mg/mL (11.48 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.2296 mL 1.1482 mL 2.2963 mL
5 mM 0.0459 mL 0.2296 mL 0.4593 mL
10 mM 0.0230 mL 0.1148 mL 0.2296 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. K McCrea, et al. 2-36[K4,RYYSA(19-23)]PP a novel Y5-receptor preferring ligand with strong stimulatory effect on food intake. Regul Pept. 2000 Feb 8;87(1-3):47-58.

    [2]. J Fuhlendorff, et al. [Leu31, Pro34]neuropeptide Y: a specific Y1 receptor agonist. Proc Natl Acad Sci U S A. 1990 Jan;87(1):182-6.

    [3]. A Kask, et al. Evidence for involvement of neuropeptide Y receptors in the regulation of food intake: studies with Y1-selective antagonist BIBP3226. Br J Pharmacol. 1998 Aug;124(7):1507-15.

D[LEU4,LYS8]-VP TFA

发表于由

D[LEU4,LYS8]-VP TFA; 纯度: 98.16%

D[LEU4,LYS8]-VP TFA 是血管加压素 V1b 受体的选择性激动剂，对大鼠，人类和小鼠 V1b 受体的 Ki 值分别为 0.16 nM，0.52 nM 和 1.38 nM。D[LEU4,LYS8]-VP TFA 具有较弱的抗利尿剂、升压药和体外催产素活性。

D[LEU4,LYS8]-VP TFAamp;;

D[LEU4,LYS8]-VP TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ￥800 In-stock
10 mg ￥1300 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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D[LEU4,LYS8]-VP TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Macrocyclic Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • Peptide Library

生物活性

D[LEU4,LYS8]-VP TFA is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP TFA has weak antidiuretic, vasopressor, and in vitro oxytocic activities[1][2].

IC50 Target

vasopressin V1b receptor[1]
分子量

1140.25

Formula

C49H68F3N11O13S2
Sequence

{Mpa}-Tyr-Phe-Leu-Asn-Cys-Pro-Lys-Gly (Disulfide bridge:Mpa1-Cys6)
Sequence Shortening

{Mpa}-YFLNCPKG-NH2 (Disulfide bridge:Mpa1-Cys6)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
Solvent Solubility
In Vitro:;

H2O

Peptide Solubility and Storage Guidelines:

1.;;Calculate the length of the peptide.

2.;;Calculate the overall charge of the entire peptide according to the following table:

; Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.;;Recommended solution:

Overall charge of peptide Details
Negative (lt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (lt;50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. Ana P, et, al. Pharmacological and physiological characterization of d[Leu4, Lys8]vasopressin, the first V1b-selective agonist for rat vasopressin/oxytocin receptors. Endocrinology. 2007 Sep; 148(9): 4136-46.

    [2]. Ana P, et, al. Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8. J Med Chem. 2007 Feb 22; 50(4): 835-47.

N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys(Synonyms: For-Nle-Leu-Phe-Nle-Tyr-Lys-OH)

发表于由

N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys;(Synonyms: For-Nle-Leu-Phe-Nle-Tyr-Lys-OH) 纯度: 98.64%

N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys TFA (For-Nle-Leu-Phe-Nle-Tyr-Lys-OH TFA) 是一种甲酰肽受体 (FPR) 激动剂。

N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lysamp;;(Synonyms: For-Nle-Leu-Phe-Nle-Tyr-Lys-OH)

N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys Chemical Structure

CAS No. : 71901-21-8

规格 价格 是否有货 数量
5 mg ￥950 In-stock
10 mg ￥1450 In-stock
25 mg ￥2450 In-stock
50 mg ￥3400 In-stock
100 mg ￥4900 询价
200 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Peptide Library

生物活性

N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys TFA (For-Nle-Leu-Phe-Nle-Tyr-Lys-OH TFA) is a formyl peptide receptor (FPR) agonist[1].

分子量

824.02

Formula

C43H65N7O9
CAS 号

71901-21-8
Sequence

N-Formyl-{NLE}-Leu-Phe-{NLE}-Tyr-Lys
Sequence Shortening

N-Formyl-{NLE}-LF-{NLE}-YK
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

H2O : 16.67 mg/mL (20.23 mM; ultrasonic and adjust pH to 12 with NaOH)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2136 mL 6.0678 mL 12.1356 mL
5 mM 0.2427 mL 1.2136 mL 2.4271 mL
10 mM 0.1214 mL 0.6068 mL 1.2136 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Stenfeldt AL, et al. The non-steroidal anti-inflammatory drug piroxicam blocks ligand binding to the formyl peptidereceptor but not the formyl peptide receptor like 1. Biochem Pharmacol. 2007 Oct 1;74(7):1050-6.

[Ala11,D-Leu15]-Orexin B(human) TFA

发表于由

[Ala11,D-Leu15]-Orexin B(human) TFA;

[Ala11,D-Leu15]-Orexin B(human) TFA 是一种有效的，选择性的 orexin-2 receptor (OX2) 的激动剂。[Ala11,D-Leu15]-Orexin B(human) TFA 对 OX2 (EC50=0.13 nM) 比对 OX1 (52 nM) 高出 400 倍的选择性。

[Ala11,D-Leu15]-Orexin B(human) TFAamp;;

[Ala11,D-Leu15]-Orexin B(human) TFA Chemical Structure

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

[Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM)[1].

IC50 Target[1]

OX2

0.13 (EC50)

OX1

52 (EC50)

分子量

2971.28

Formula

C122H207F3N44O37S
Sequence

Arg-Ser-Gly-Pro-Pro-Gly-Leu-Gln-Gly-Arg-Ala-Gln-Arg-Leu-Leu-Gln-Ala-Ser-Gly-Asn-His-Ala-Ala-Gly-Ile-Leu-Thr-Met-NH2
Sequence Shortening

RSGPPGLQGRAQRLLQASGNHAAGILTM-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Asahi S, et al. Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B. Bioorg Med Chem Lett. 2003;13(1):111-113.