Transdermal Peptide Disulfide TFA(Synonyms: TD 1 Disulfide(peptide) TFA)

Transdermal Peptide Disulfide TFA;(Synonyms: TD 1 Disulfide(peptide) TFA) 纯度: 98.45%

Transdermal Peptide Disulfide TFA (TD 1 Disulfide(peptide) TFA) 是由 11 个氨基酸组成的多肽,可以与 Na+/K+-ATPase beta-subunit (ATP1B1) 结合,主要与 ATP1B1 的 C 末端相互作用。Transdermal Peptide Disulfide TFA 能够增强一些大分子在皮肤中的传递。

Transdermal Peptide Disulfide TFAamp;;(Synonyms: TD 1 Disulfide(peptide) TFA)

Transdermal Peptide Disulfide TFA Chemical Structure

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1 mg ¥800 In-stock
5 mg ¥1800 In-stock
10 mg ¥2800 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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Transdermal Peptide Disulfide TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library
  • Peptide Library

生物活性

Transdermal Peptide Disulfide TFA (TD 1 Disulfide(peptide) TFA) is a 11-amino acid peptide, binds to Na+/K+-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide TFA can enhance the transdermal delivery of many macromolecules[1].

体外研究
(In Vitro)

In the presence of Transdermal Peptide Disulfide, because of the specific binding of Transdermal Peptide Disulfide to ATP1B1, cells will upregulate the level of ATP1B1 to maintain function and structure; as a result, the expression of ATP1B1 increases. However, as time goes on, some Transdermal Peptide Disulfide molecules may be transported into cells by endocytosis; consequently, the expression of ATP1B1 then decreases. The interaction between Transdermal Peptide Disulfide and ATP1B1 changes not only the expression of ATP1B1, but also the localization of ATP1B1 and then the structure of the epidermal layer. This interaction can be attenuated by inhibitors or competitors, which would result in the reduced delivery of macromolecular drugs across the skin[1].

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

分子量

1175.17

Formula

C42H65F3N14O18S2

Sequence Shortening

ACSSSPSKHCG (Disulfide bridge: Cys2-Cys10)

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 : 100 mg/mL (85.09 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8509 mL 4.2547 mL 8.5094 mL
5 mM 0.1702 mL 0.8509 mL 1.7019 mL
10 mM 0.0851 mL 0.4255 mL 0.8509 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]. Wang C, et al. Role of the Na(+)/K(+)-ATPase beta-subunit in peptide-mediated transdermal drug delivery. Mol Pharm. 2015 Apr 6;12(4):1259-67.

β-Casomorphin, human TFA(Synonyms: Human β-casomorphin 7 TFA)

β-Casomorphin, human TFA;(Synonyms: Human β-casomorphin 7 TFA) 纯度: 99.67%

β-Casomorphin, human TFA (Human β-casomorphin 7 TFA) 是一种阿片样肽,作为 opioid 受体激动剂。

β-Casomorphin, human TFAamp;;(Synonyms: Human β-casomorphin 7 TFA)

β-Casomorphin, human TFA Chemical Structure

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5 mg ¥1500 In-stock
10 mg ¥2500 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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beta;-Casomorphin, human TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Neuronal Signaling Compound Library
  • Neurotransmitter Receptor Compound Library
  • Peptide Library

生物活性

β-Casomorphin, human TFA (Human β-casomorphin 7 TFA) is an opioid peptide, acts as an agonist of opioid receptor[1][2].

IC50 Target

Opioid receptor[2]

体外研究
(In Vitro)

β-Casomorphin, human TFA induces contractions of the guinea-pig ileum myenteric plexus/longitudinal muscle preparation with an IC50 of 29 μM[1].
β-Casomorphin, human TFA displaces 3H-spiperone from receptors in frontal cortex starting with 500 nM concentrations[2].

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

分子量

978.02

Formula

C46H62F3N7O13

Sequence

Tyr-Pro-Phe-Val-Glu-Pro-Ile

Sequence Shortening

YPFVEPI

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:;

DMSO : 100 mg/mL (102.25 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0225 mL 5.1124 mL 10.2247 mL
5 mM 0.2045 mL 1.0225 mL 2.0449 mL
10 mM 0.1022 mL 0.5112 mL 1.0225 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。

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 (2.56 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.56 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 (2.56 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.56 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 (2.56 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.56 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]. Brantl V. Novel opioid peptides derived from human beta-casein: human beta-casomorphins. Eur J Pharmacol. 1984 Oct 30;106(1):213-4.

    [2]. Koch G, et al. Opioid activities of human beta-casomorphins. Naunyn Schmiedebergs Arch Pharmacol. 1985 Dec;331(4):351-4.

HS024 TFA

HS024 TFA; 纯度: 99.63%

HS024 是一种选择性的 MC4 受体拮抗剂,对 MC4、MC5、MC3 和 MC1 的 Ki 分别为 0.29、3.29、5.45 和 18.6 nM。HS024 增加食物摄入。

HS024 TFAamp;;

HS024 TFA Chemical Structure

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1 mg ¥1400 In-stock
5 mg ¥3200 In-stock
10 mg ¥5200 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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HS024 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Neuronal Signaling Compound Library
  • Peptide Library

生物活性

HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake[1].

分子量

1380.52

Formula

C60H80F3N19O12S2

Sequence Shortening

Ac-C-{Nle}-RH-{D-2Nal}-RWGC-NH2 (Disulfide bridge:Cys1-Cys9)

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 (36.22 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7244 mL 3.6218 mL 7.2436 mL
5 mM 0.1449 mL 0.7244 mL 1.4487 mL
10 mM 0.0724 mL 0.3622 mL 0.7244 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]. Kask A, et al. Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): evaluation in vitro and in vivo. Endocrinology. 1998;139(12):5006-5014.

PBP10 TFA

PBP10 TFA; 纯度: 98.47%

PBP10 是一种甲酰基肽受体 2 (FPR2) 的细胞通透性和选择性的由 gelsolin 衍生的肽抑制剂,选择性优于对 FPR1 的。PBP10 是一种 N 端偶联罗丹明的10 个氨基酸的肽,对革兰氏阳性和革兰氏阴性菌具有杀菌活性,并且可以限制微生物诱导的炎症作用。

PBP10 TFAamp;;

PBP10 TFA Chemical Structure

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5 mg ¥4200 In-stock
10 mg ¥6700 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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PBP10 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Immunology/Inflammation Compound Library
  • Antibacterial Compound Library
  • Peptide Library

生物活性

PBP10 is a cell permeable and selective gelsolin-derived peptide inhibitor of formyl peptide receptor 2 (FPR2) over FPR1[1]. PBP10 is a 10-AA peptide with rhodamine conjugated at its N terminus, exerts bactericidal activity against gram-positive and gram-negative bacteria and limits microbial-induced inflammatory effects[2].

IC50 Target

IC50: formyl peptide receptor 2 (FPR2)[1]

分子量

1827.08

Formula

C86H128F3N24O17

Sequence

RhB-Gln-Arg-Leu-Phe-Gln-Val-Lys-Gly-Arg-Arg-OH

Sequence Shortening

RhB-QRLFQVKGRR-OH

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 : 7.14 mg/mL (3.91 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.5473 mL 2.7366 mL 5.4732 mL
5 mM
10 mM

*

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]. Ewelina Piktel, et al. Inhibition of inflammatory response in human keratinocytes by magnetic nanoparticles functionalized with PBP10 peptide derived from the PIP2-binding site of human plasma gelsolin. J Nanobiotechnology. 2019 Feb 2;17(1):22.

    [2]. C C Cunningham, et al.Cell permeant polyphosphoinositide-binding peptides that block cell motility and actin assembly. J Biol Chem

TAT-DEF-Elk-1 TFA(Synonyms: TDE TFA)

TAT-DEF-Elk-1 TFA;(Synonyms: TDE TFA)

TAT-DEF-Elk-1 TFA (TDE TFA) 是 Elk-1 的一种可穿透细胞的肽抑制剂,通过模仿和特异性干扰 Elk-1 的 DEF 结构域来实现抑制。TAT-DEF-Elk-1 TFA 阻止 Elk-1 磷酸化并防止 Elk-1 核易位,且不会干扰 ERK 或 MSK1 活化。TAT-DEF-Elk-1 TFA 是分析神经元可塑性发展过程中 Elk-1 在此过程中的作用的有用工具。

TAT-DEF-Elk-1 TFAamp;;(Synonyms: TDE TFA)

TAT-DEF-Elk-1 TFA Chemical Structure

规格 价格 是否有货
1 mg ¥1500 询问价格 货期
5 mg ¥4500 询问价格 货期
10 mg ¥7500 询问价格 货期

* Please select Quantity before adding items.

生物活性

TAT-DEF-Elk-1 TFA (TDE TFA) is a cell-penetrating peptide inhibitor of Elk-1, mimics and specifically interferes with the DEF domain of Elk-1. TAT-DEF-Elk-1 TFA blocks Elk-1 phosphorylation and prevents Elk-1 nuclear translocation without interfering with ERK nor MSK1 activation. TAT-DEF-Elk-1 TFA is a useful tool to analyze the role of Elk-1 in this process during the development of neuronal plasticity[1].

IC50 Target

IC50: Elk-1[1]

体外研究
(In Vitro)

Elk-1 phosphorylation on Ser383/389 has a dual function and triggers both Elk-1 nuclear translocation and SRE-dependent gene expression[1].
TAT-DEF-Elk-1 TFA (5 μM; 1 hour) specifically inhibits glutamate-induced elk-1 activation and does not interfer with ERK, MSK-1, or CREB phosphorylation[1].
TAT-DEF-Elk-1 TFA (5-10 μM; 2 hour) treatment shows a significant inhibition of c-Fos, Zif268 and JunB, but has no effects on c-Jun expression[1].

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

Western Blot Analysis[2]

Cell Line: Neurons
Concentration: 5 μM; 10 μM
Incubation Time: 1 hour
Result: Decreased elk-1 expression and had no effects on ERK, MSK-1, or CREB phosphorylation.

RT-PCR[2]

Cell Line: Primary striatal neurons
Concentration: 5 μM
Incubation Time: 2 hour
Result: Decreased c-Fos, Zif268 and JunB mRNA level but did not effect c-Jun.

体内研究
(In Vivo)

TAT-DEF-Elk-1 TFA (intraperitoneal injection; 1mg/kg; daily; 14 days) reflects antidepressant efficacy in mice, it decreases immobility similar to the reference antidepressants fluoxetine and desipramine (DMI)[1].

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

Animal Model: C57Bl6 mice (3-6 months old males) are subjected to social defeat stress[2]
Dosage: 1 mg/kg
Administration: Intraperitoneal injection; daily; 14 days
Result: Reversed social-defeat induced decrease of hippocampal Bdnf expression by repeated TDE administration.

分子量

3675.09

Formula

C157H260N57F3O42

Sequence

Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Pro-Pro-Ser-Pro-Ala-Lys-Leu-Ser-Phe-Gln-Phe-Pro-Ser-Ser-Gly-Ser-Ala-Gln-Val-His-Ile

Sequence Shortening

GRKKRRQRRRPPSPAKLSFQFPSSGSAQVHI

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)

参考文献
  • [1]. Lavaur J, et al. A TAT-DEF-Elk-1 peptide regulates the cytonuclear trafficking of Elk-1 and controls cytoskeleton dynamics.J Neurosci. 2007 Dec 26;27(52):14448-58.

    [2]. Apazoglou K, et al. Antidepressive effects of targeting ELK-1 signal transduction.Nat Med. 2018 May;24(5):591-597.

UFP-101 TFA

UFP-101 TFA; 纯度: 99.36%

UFP-101 TFA 是一种强效、选择性和竞争性的 NOP 受体拮抗剂,pKi 为 10.24。UFP-101 TFA 对 δ、μ 和 κ 类阿片受体的选择性大于 3000 倍。UFP-101 TFA 具有抗抑郁药样作用。

UFP-101 TFAamp;;

UFP-101 TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ¥3500 In-stock
5 mg ¥10000 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

UFP-101 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect[1][2].

体内研究
(In Vivo)

UFP-101 TFA elicits a pronounced acute and dosedependent antidepressant-like effect in mice submitted to the forced swimming test (FST)[1].

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

分子量

2022.19

Formula

C84H139F3N32O23

Sequence Shortening

Bn-GGGFTGARKSARKRKNQ-NH2

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:;

H2O : 130 mg/mL (64.29 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.4945 mL 2.4726 mL 4.9451 mL
5 mM 0.0989 mL 0.4945 mL 0.9890 mL
10 mM 0.0495 mL 0.2473 mL 0.4945 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。

参考文献
  • [1]. Calo G, et al. [Nphe1,Arg14,Lys15]nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor. Br J Pharmacol. 2002;136(2):303-311.

    [2]. Gavioli EC, et al. Blockade of nociceptin/orphanin FQ-NOP receptor signalling produces antidepressant-like effects: pharmacological and genetic evidences from the mouse forced swimming test. Eur J Neurosci. 2003;17(9):1987-1990.

Z-VRPR-FMK TFA(Synonyms: VRPR)

Z-VRPR-FMK TFA;(Synonyms: VRPR) 纯度: 95.92%

Z-VRPR-FMK (TFA) (VRPR) 是一种四肽,也是选择性和不可逆的粘膜相关淋巴组织淋巴瘤易位蛋白1 (MALT1) 抑制剂。Z-VRPR-FMK (TFA) 有抗甲型流感病毒 (IAV) 感染的作用。

Z-VRPR-FMK TFAamp;;(Synonyms: VRPR)

Z-VRPR-FMK TFA Chemical Structure

规格 价格 是否有货 数量
500 μg ¥7800 In-stock

* Please select Quantity before adding items.

生物活性

Z-VRPR-FMK (TFA) (VRPR), a tetrapeptide, is a selective and irreversible MALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1) inhibitor. Z-VRPR-FMK (TFA) can protect against influenza A virus (IAV) infection[1].

分子量

790.81

Formula

C33H50F4N10O8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Pure form -80deg;C 2 years
-20deg;C 1 year

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

参考文献
  • [1]. Hatcher JM, et al. Peptide-based covalent inhibitors of MALT1 paracaspase. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1336-1339.

Urotensin I TFA(Synonyms: Catostomus urotensin I TFA)

Urotensin I TFA;(Synonyms: Catostomus urotensin I TFA) 纯度: 98.29%

Urotensin I (Catostomus urotensin I) TFA 是一种类 CRF 样肽,可作为 CRF 受体激动剂,在细胞实验中,对人 CRF1,CRF2 和大鼠 CRF 受体的 pEC50 值分别为 11.46,9.36 和 9.85,对 hCRF1,rCRF 和 mCRF 受体的 Ki 值分别为 0.4,1.8 和 5.7 nM。

Urotensin I TFAamp;;(Synonyms: Catostomus urotensin I TFA)

Urotensin I TFA Chemical Structure

规格 价格 是否有货 数量
500 μg ¥3400 In-stock

* Please select Quantity before adding items.

Urotensin I TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Urotensin I (Catostomus urotensin I) TFA, a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF and mCRF receptors, respectively[1][2].

IC50 Target

pEC50: 11.46 (human CRF1, CHO cells), 9.36 (human CRF2, CHO cells), 9.85 (rat CRF, CHO cells)[1]
Ki: 0.4 nM (hCRF1, cell assay), 1.8 nM (rCRF, cell assay), and 5.7 nM (mCRF, cell assay)[2]

体外研究
(In Vitro)

Urotensin I is 2-3 times more potent than CRF or sauvagine in stimulating ACTH release from a superfused goldfish anterior pituitary cell column[3].
Rat tail artery strips were incubated in the presence of 4 x 10(-3) M theophylline and Urotensin I (UI). At the concentrations of 1.50, 7.50 mU/ml but not of 0.75 mU/ml Urotensin I, the content of cAMP increased significantly[4].

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

体内研究
(In Vivo)

Intraperitoneal injections of urotensin I, a CRF-like neuropeptide isolated from the caudal neurosecretory system of the teleost Catostomus commersoni, ovine CRF and sauvagine all produced significant increases in circulating levels of plasma cortisol in goldfish in which endogenous ACTH secretion was suppressed with betamethasone[3].

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

分子量

4983.48

Formula

C212H341F3N62O69S2

Sequence

Asn-Asp-Asp-Pro-Pro-Ile-Ser-Ile-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Asn-Met-Ile-Glu-Met-Ala-Arg-Ile-Glu-Asn-Glu-Arg-Glu-Gln-Ala-Gly-Leu-Asn-Arg-Lys-Tyr-Leu-Asp-Glu-Val-NH2

Sequence Shortening

NDDPPISIDLTFHLLRNMIEMARIENEREQAGLNRKYLDEV-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)

参考文献
  • [1]. Smart D, et al. Characterisation using microphysiometry of CRF receptor pharmacology. Eur J Pharmacol. 1999 Aug 27;379(2-3):229-35.

    [2]. Reul JM, et al. Corticotropin-releasing factor receptors 1 and 2 in anxiety and depression. Curr Opin Pharmacol. 2002 Feb;2(1):23-33.

    [3]. Fryer J, et al. Urotensin I, a CRF-like neuropeptide, stimulates acth release from the teleost pituitary. Endocrinology. 1983;113(6):2308-2310.

    [4]. Gerritsen ME, et al. Urotensin I effects on intracellular content of cyclic AMP in the rat tail artery. Eur J Pharmacol. 1979;60(2-3):211-220.

Saralasin TFA(Synonyms: [Sar1,Ala8] Angiotensin II TFA)

Saralasin TFA;(Synonyms: [Sar1,Ala8] Angiotensin II TFA) 纯度: 99.18%

Saralasin ([Sar1,Ala8] Angiotensin II) TFA 是一种竞争性血管紧张素II (angiotensin II) 拮抗剂。Saralasin-TFA 被用来鉴别肾素依赖性 (血管紧张素原性) 高血压。

Saralasin TFAamp;;(Synonyms: [Sar1,Ala8] Angiotensin II TFA)

Saralasin TFA Chemical Structure

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ¥6550 In-stock
5 mg ¥3500 In-stock
10 mg ¥5800 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

Saralasin TFA 相关产品

bull;相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • FDA-Approved Drug Library
  • Drug Repurposing Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • Neurotransmitter Receptor Compound Library
  • FDA Approved amp; Pharmacopeial Drug Library
  • Angiogenesis Related Compound Library
  • Peptide Library

生物活性

Saralasin ([Sar1,Ala8] Angiotensin II) TFA is a competitive angiotensin II antagonist. Saralasin TFA is used to identify renin-dependent (angiotensinogenic) hypertension[1].

体外研究
(In Vitro)

Saralasin ([Sar1,Ala8] Angiotensin II) TFA is an intravenously administered, competitive antagonist of angiotensin II that is used to identify renin-dependent (angiotensinogenic) hypertension[1].
Saralasin TFA (1 nmol/ml) inhibits cell growth in 3T3 and SV3T3 cells and causes an increase of cellular renin concentration[2].

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

体内研究
(In Vivo)

Saralasin ([Sar1,Ala8] Angiotensin II) TFA (10 and 30 mg/kg) increases serum renin activity (SRA) in normal, conscious rats from 2.7 to 16.2 and 22.5 ng/ml/hr, respectively, without markedly altering blood pressure or heart rate. n sodium-depleted rats, Saralasin TFA (0.3 mg/kg) increased SRA from 12 to 119 ng/ml/hr and decreased blood pressure by 6%[3].

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

分子量

1026.07

Formula

C44H66F3N13O12

Sequence

{Sar}-Arg-Val-Tyr-Val-His-Pro-Ala

Sequence Shortening

{Sar}-RVYVHPA

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:;

DMSO : 50 mg/mL (48.73 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9746 mL 4.8730 mL 9.7459 mL
5 mM 0.1949 mL 0.9746 mL 1.9492 mL
10 mM 0.0975 mL 0.4873 mL 0.9746 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。

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 (2.44 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.44 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 (2.44 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.44 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 (2.44 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.44 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]. Weber MA. Saralasin testing for renin-dependent hypertension. Arch Intern Med. 1979;139(1):93‐95.

    [2]. Schelling P, Ganten D, Speck G, Fischer H. Effects of angiotensin II and angiotensin II antagonist saralasin on cell growth and renin in 3T3 and SV3T3 cells. J Cell Physiol. 1979;98(3):503‐513.

    [3]. Campbell WB, Jackson EK, Graham RM. Saralasin-induced renin release: its blockade by prostaglandin synthesis inhibitors in the conscious rat. Hypertension. 1979;1(6):637‐642.

Echistatin TFA

Echistatin TFA; 纯度: 95.13%

Echistatin TFA 最初是来自蛇毒崩素家族中最小的 RGD 活性蛋白,是一种有效的血小板聚集的抑制剂。Echistatin 是体外骨吸收的有效抑制剂。Echistatin 是有效的αIIbβ3αvβ3α5β1 的拮抗剂。

Echistatin TFAamp;;

Echistatin TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ¥10500 In-stock
5 mg ¥31500 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

Echistatin TFA 相关产品

bull;相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1[1][2][3][4].

IC50 Target[4]

αvβ3

;

α5β1

;

αIIbβ3

;

分子量

5531.02

Formula

C219H342F3N71O76S9

Sequence Shortening

ECESGPCCRNCKFLKEGTICKRARGDDMDDYCNGKTCDCPRNPHKGPAT (Disulfide bridge:Cys2-Cys11;Cys7-Cys32;Cys8-Cys37;Cys20-Cys39)

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 (9.04 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.1808 mL 0.9040 mL 1.8080 mL
5 mM 0.0362 mL 0.1808 mL 0.3616 mL
10 mM

*

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]. J Musial, et al. Inhibition of platelet adhesion to surfaces of extracorporeal circuits by disintegrins. RGD-containing peptides from viper venoms. Circulation. 1990 Jul;82(1):261-73.

    [2]. M Sato, et al. Echistatin is a potent inhibitor of bone resorption in culture. J Cell Biol. 1990 Oct;111(4):1713-23.

    [3]. C C Kumar, et al. Biochemical characterization of the binding of echistatin to integrin alphavbeta3 receptor. J Pharmacol Exp Ther. 1997 Nov;283(2):843-53.

    [4]. I Wierzbicka-Patynowski, et al. Structural requirements of echistatin for the recognition of alpha(v)beta(3) and alpha(5)beta(1) integrins. J Biol Chem. 1999 Dec 31;274(53):37809-14.