标签归档：nh

NH2-KLGADTDGEQDQHMTYGGQ-COOH

发表于由

NH2-KLGADTDGEQDQHMTYGGQ-COOH; 纯度: 98.52%

NH2-KLGADTDGEQDQHMTYGGQ-COOH 是一个合成肽链，具有连接到谷氨酰胺的羧基和与赖氨酸连接的胺基。

NH2-KLGADTDGEQDQHMTYGGQ-COOHamp;;

NH2-KLGADTDGEQDQHMTYGGQ-COOH Chemical Structure

规格 价格 是否有货 数量
1 mg ￥1100 In-stock
5 mg ￥3300 In-stock
10 mg ￥4600 In-stock
50 mg ￥11000 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

* Please select Quantity before adding items.

NH2-KLGADTDGEQDQHMTYGGQ-COOH 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

NH2-QGGYTMHQDQEGDTDAGLK-COOH is a synthetic peptide chain with an amine group attached to lysine and an carboxyl group attached to glutamine.

分子量

2051.11

Formula

C83H127N25O34S
Sequence

Lys-Leu-Gly-Ala-Asp-Thr-Asp-Gly-Glu-Gln-Asp-Gln-His-Met-Thr-Tyr-Gly-Gly-Gln
Sequence Shortening

KLGADTDGEQDQHMTYGGQ
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 : 25 mg/mL (12.19 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.4875 mL 2.4377 mL 4.8754 mL
5 mM 0.0975 mL 0.4875 mL 0.9751 mL
10 mM 0.0488 mL 0.2438 mL 0.4875 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。

TFLLR-NH2

发表于由

TFLLR-NH2;

TFLLR-NH2是选择性的PAR1激动剂，EC50值为1.9 μM。

TFLLR-NH2amp;;

TFLLR-NH2 Chemical Structure

CAS No. : 197794-83-5

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

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TFLLR-NH2 的其他形式现货产品:

TFLLR-NH2(TFA)

生物活性

TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM.

IC50 Target

EC50: 1.9 μM (PAR1)[1]
体外研究
(In Vitro)

PAR1 agonists stimulate concentration-dependent increases in [Ca2+]i and in the proportions of neurones. The maximal increase in [Ca2+]i above basal is detected in response to 10 μm TF-NH2(peak 196.5±20.4 nM, n=25) when 50–80% of identified neurones responded[1]. SW620 cells cultured in the supernatant of TFLLR-NH2-activated platelets upregulate E-cadherin expression and downregulate the vimentin expression. In the in vitro platelet culture system, a TFLLR-NH2 dose-dependent increase of secreted TGF-β1 is detected in the supernatant[2].

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

Injection of TF-NH2 into the rat paw stimulates a marked and sustained oedema. An NK1R antagonist and ablation of sensory nerves with capsaicin inhibit oedema by 44% at 1 h and completely by 5 h. In wild-type but not PAR1−/− mice, TF-NH2 stimulates Evans blue extravasation in the bladder, oesophagus, stomach, intestine and pancreas by 2–8 fold. Extravasation in the bladder, oesophagus and stomach is abolished by an NK1R antagonist[1]. TFp-NH2 produces notable contraction at 3-50 μM and relaxation at 0.3-50 μM, in the absence of apamin. The concentration-response curve for TFp-NH2-induced contraction is remarkably shifted left, when the TFp-NH2-induced relaxation is blocked by apamin at 0.1 μM[3].

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

647.81

Formula

C31H53N9O6
CAS 号

197794-83-5
Sequence

Thr-Phe-Leu-Leu-Arg-NH2
Sequence Shortening

TFLLR-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]. de Garavilla L, et al. Agonists of proteinase-activated receptor 1 induce plasma extravasation by a neurogenic mechanism. Br J Pharmacol. 2001 Aug;133(7):975-87.

    [2]. Kawabata A, et al. Characterization of the protease-activated receptor-1-mediated contraction and relaxation in the rat duodenal smooth muscle.

    [3]. Jia Y, et al. Activation of platelet protease-activated receptor-1 induces epithelial-mesenchymal transition and chemotaxis of colon cancer cell line SW620. Oncol Rep. 2015 Jun;33(6):2681-8.
Animal Administration
[1]

Mice: Mice are anaesthetized with isofluorane, and saline or TF-NH2 (3 μmol/kg in 25 μL physiological saline) is injected into the lateral tail vein. Evans blue (33.3 mg/kg in 50 μL saline) is co-injected with the peptide. Mice are perfused transcardially at 10 min after administration of TF-NH2 with physiological saline containing 20 u/mL heparin at a pressure of 80-100 mmHg for 2-3 min. Excised tissues are incubated in 1 mL of formamide for 48 h, and Evans blue content is measured spectrophotometrically at 650 nm[1].

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

  • [1]. de Garavilla L, et al. Agonists of proteinase-activated receptor 1 induce plasma extravasation by a neurogenic mechanism. Br J Pharmacol. 2001 Aug;133(7):975-87.

    [2]. Kawabata A, et al. Characterization of the protease-activated receptor-1-mediated contraction and relaxation in the rat duodenal smooth muscle.

    [3]. Jia Y, et al. Activation of platelet protease-activated receptor-1 induces epithelial-mesenchymal transition and chemotaxis of colon cancer cell line SW620. Oncol Rep. 2015 Jun;33(6):2681-8.

LRGILS-NH2 TFA

发表于由

LRGILS-NH2 TFA; 纯度: 98.15%

LRGILS-NH2 TFA 是一个反向序列蛋白酶激活受体-2 (PAR-2) 不活跃的，阴性对照。SLIGRL-NH2 则是 PAR-2 激活肽。

LRGILS-NH2 TFAamp;;

LRGILS-NH2 TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ￥600 In-stock
5 mg ￥1800 In-stock
10 mg ￥2900 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

LRGILS-NH2 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

LRGILS-NH2 TFA is a reverse-sequence protease-activated receptor-2 (PAR-2)-inactive, negative control, and SLIGRL-NH2 is a PAR-2-activating peptide[1].

分子量

770.84

Formula

C31H57F3N10O9
Sequence Shortening

LRGILS-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:;

DMSO : ≥ 100 mg/mL (129.73 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 1.2973 mL 6.4864 mL 12.9729 mL
5 mM 0.2595 mL 1.2973 mL 2.5946 mL
10 mM 0.1297 mL 0.6486 mL 1.2973 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 ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.24 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
*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Nishikawa H, Kawai K, Tanaka M, et al. Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: involvement of PAR-2 and non-PAR-2 mechanisms. J Pharmacol Exp Ther. 2005;312(1):324-331.

VKGILS-NH2

发表于由

VKGILS-NH2; 纯度: 99.68%

VKGILS-NH2 是一种 SLIGKV-NH2 (蛋白酶激活的受体 2 (PAR2) 的激动剂) 的反向氨基酸序列对照肽，对细胞中的 DNA 合成没有影响。

VKGILS-NH2amp;;

VKGILS-NH2 Chemical Structure

CAS No. : 942413-05-0

规格 价格 是否有货 数量
5 mg ￥1200 In-stock
10 mg ￥2000 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

VKGILS-NH2 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Peptide Library

生物活性

VKGILS-NH2 is a reversed amino acid sequence control peptide for SLIGKV-NH2 (protease-activated receptor 2 (PAR2) agonist). VKGILS-NH2 has no effect on DNA synthesis in cells[1][2].

分子量

614.78

Formula

C28H54N8O7
CAS 号

942413-05-0
Sequence

Val-Lys-Gly-Ile-Leu-Ser-NH2
Sequence Shortening

VKGILS-NH2
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 (162.66 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6266 mL 8.1330 mL 16.2660 mL
5 mM 0.3253 mL 1.6266 mL 3.2532 mL
10 mM 0.1627 mL 0.8133 mL 1.6266 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: ≥ 2.5 mg/mL (4.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.07 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 (4.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.07 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 (4.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.07 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]. M Tognetto, et al. Evidence That PAR-1 and PAR-2 Mediate Prostanoid-Dependent Contraction in Isolated Guinea-Pig Gallbladder. Br J Pharmacol. 2000 Oct;131(4):689-94.

    [2]. David A Vesey, et al. Proinflammatory and Proliferative Responses of Human Proximal Tubule Cells to PAR-2 Activation. Am J Physiol Renal Physiol. 2007 Nov;293(5):F1441-9.

VKGILS-NH2 TFA

发表于由

VKGILS-NH2 TFA;

VKGILS-NH2 TFA 是一种 SLIGKV-NH2 (蛋白酶激活的受体 2 (PAR2) 的激动剂) 的反向氨基酸序列对照肽，对细胞中的 DNA 合成没有影响。

VKGILS-NH2 TFAamp;;

VKGILS-NH2 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.

VKGILS-NH2 TFA 的其他形式现货产品:

VKGILS-NH2

生物活性

VKGILS-NH2 TFA is a reversed amino acid sequence control peptide for SLIGKV-NH2 (protease-activated receptor 2 (PAR2) agonist). VKGILS-NH2 TFA has no effect on DNA synthesis in cells[1][2].

分子量

728.80

Formula

C30H55F3N8O9
Sequence

Val-Lys-Gly-Ile-Leu-Ser-NH2
Sequence Shortening

VKGILS-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]. M Tognetto, et al. Evidence That PAR-1 and PAR-2 Mediate Prostanoid-Dependent Contraction in Isolated Guinea-Pig Gallbladder. Br J Pharmacol. 2000 Oct;131(4):689-94.

    [2]. David A Vesey, et al. Proinflammatory and Proliferative Responses of Human Proximal Tubule Cells to PAR-2 Activation. Am J Physiol Renal Physiol. 2007 Nov;293(5):F1441-9.

Ac-RYYRWK-NH2 TFA

发表于由

Ac-RYYRWK-NH2 TFA;

Ac-RYYRWK-NH2 TFA 是一个有效的和选择性 nociceptin receptor (NOP) 部分激动剂。[3H]Ac-RYYRWK-NH2 TFA 结合鼠皮层膜的 ORL1 的Kd 为0.071 nM，但是对 µ-,κ- 或 δ 阿片受体没有亲和力。

Ac-RYYRWK-NH2 TFAamp;;

Ac-RYYRWK-NH2 TFA Chemical Structure

CAS No. : 408305-09-9

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

Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors[1].

体外研究
(In Vitro)

[3H]ac-RYYRWK-NH2 binding to rat cortical membranes revealed a single high affinity site for [3H]ac-RYYRWK-NH2 (Kd=0.071 nM)[1].
Naloxone benzoylhydrazone displaced [3H]acRYYRWK-NH2 binding to rat cortical membranes (Ki=104 nM) and human ORL1 (Ki=136 nM) as well as [125I]Tyr14-NC-OH to ORL1 (Ki=37 nM) has no affinity for µ-, κ- or δ-opioid receptors[1].

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

1126.19

Formula

C51H70F3N15O11
CAS 号

408305-09-9
Sequence Shortening

Ac-RYYRWK-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]. C T Dooley, et al. Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.J Pharmacol Exp Ther. 1997 Nov;283(2):735-41.

    [2]. M Ho, et al, Characterization of the ORL(1) receptor on adrenergic nerves in the rat anococcygeus muscle. Br J Pharmacol. 2000 Sep;131(2):349-55.

RLLFT-NH2 TFA

发表于由

RLLFT-NH2 TFA;

RLLFT-NH2 TFA 是一种 TFLLR-NH2 的反向氨基酸序列阴性对照肽。

RLLFT-NH2 TFAamp;;

RLLFT-NH2 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

RLLFT-NH2 TFA is a reversed amino acid sequence negative control peptide for TFLLR-NH2[1].

分子量

761.83

Formula

C33H54F3N9O8
Sequence

Arg-Leu-Leu-Phe-Thr-NH2
Sequence Shortening

RLLFT-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]. Michelle C Buresi, et al. Activation of Proteinase-Activated receptor-1 Inhibits Neurally Evoked Chloride Secretion in the Mouse Colon in Vitro. Am J Physiol Gastrointest Liver Physiol. 2005 Feb;288(2):G337-45.

HSDVHK-NH2 TFA

发表于由

HSDVHK-NH2 TFA;

HSDVHK-NH2 TFA 是整合素 αvβ3-玻璃体结合蛋白的互作拮抗剂，其 IC50 值为 1.74 pg/mL (2.414 pM)。

HSDVHK-NH2 TFAamp;;

HSDVHK-NH2 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.

HSDVHK-NH2 TFA 的其他形式现货产品:

HSDVHK-NH2

生物活性

HSDVHK-NH2 TFA is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM)[1][2].

体外研究
(In Vitro)

HSDVHK significantly inhibited bFGF-induced cell migration compared to the PBS control group[1].
The Arg-Gly-Asp (RGD)-binding site recognition by HSDVHK-NH2 (P11) is site specific because the HSDVHK-NH2 (P11) is inactive for the complex formation of a denatured form of integrin–vitronectin. HSDVHK-NH2 (P11) shows a strong antagonism against avb3-GRGDSP interaction with an IC50 value of 25.72 nM[2].
HSDVHK-NH2 (P11) inhibits the HUVEC proliferation due to the induction of HUVEC cell death through caspases activations and its mechanism is related with increased p53 expression[3].

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

Cell Proliferation Assay[3]

Cell Line: HUVEC cells.
Concentration: 0.1, 1, 10, and 100 μg/mL.
Incubation Time: 72 h.
Result: Significantly inhibited HUVEC proliferation on denatured collagen-coated plates in a dose-dependent manner.

分子量

834.80

Formula

C32H49F3N12O11
Sequence Shortening

HSDVHK-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.
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]. Yoonsuk Lee, et al. High-throughput screening of novel peptide inhibitors of an integrin receptor from the hexapeptide library by using a protein microarray chip. J Biomol Screen. 2004 Dec;9(8):687-94.

    [2]. Youngjin Choi, et al. Site-specific inhibition of integrin alpha v beta 3-vitronectin association by a ser-asp-val sequence through an Arg-Gly-Asp-binding site of the integrin. Proteomics. 2010 Jan;10(1):72-80.

    [3]. Ji-Young Bang, et al. Pharmacoproteomic analysis of a novel cell-permeable peptide inhibitor of tumor-induced angiogenesis. Mol Cell Proteomics. 2011 Aug;10(8):M110.005264.

Ac-RYYRIK-NH2 TFA

发表于由

Ac-RYYRIK-NH2 TFA;

Ac-RYYRIK-NH2 TFA 是一种有效的 ORL1 部分激动剂，作为 ORL1 的内源性配体，在 CHO 细胞中 (Kd=1.5 nM)。Ac-RYYRIK-NH2 TFA 是 G 蛋白激活的特异性拮抗剂，竞争性拮抗 noc/OFQ 在大鼠脑膜和脑切面刺激 [35S]-GTPgS 结合 G 蛋白。

Ac-RYYRIK-NH2 TFAamp;;

Ac-RYYRIK-NH2 TFA Chemical Structure

规格 是否有货
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生物活性

Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain[1].

IC50 Target

Kd: 1.5 nM (ORL1 in CHO cells)[1]
体内研究
(In Vivo)

Ac-RYYRIK-NH2 TFA (intracerebroventricularly (i.c.v.)) inhibits spontaneous locomotor activity in mice with an ID50 of 0.07 nmol. Co-administration of noc/OFQ and Ac-RYYRIK-NH2 lead to additive effects in Male Swiss mice[1].

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

1053.13

Formula

C46H71F3N14O11
Sequence Shortening

Ac-RYYRIK-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]. H Berger, et al. Antagonism by acetyl-RYYRIK-NH2 of G protein activation in rat brain preparations and of chronotropic effect on rat cardiomyocytes evoked by nociceptin/orphanin FQ. Br J Pharmacol. 1999 Feb;126(3):555-8.

    [2]. H Berger, et al. The nociceptin/orphanin FQ receptor ligand acetyl-RYYRIK-amide exhibits antagonistic and agonistic properties.Peptides. 2000 Jul;21(7):1131-9.

    [3]. C T Dooley, et al. Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1. J Pharmacol Exp Ther. 1997 Nov;283(2):735-41.

K-(D-1-Nal)-FwLL-NH2

发表于由

K-(D-1-Nal)-FwLL-NH2;

K-(D-1-Nal)-FwLL-NH2 是一种高亲和力、强效、反向的 ghrelin receptor 激动剂 (EC50=3.4 nM； Ki=4.9 nM)。K-(D-1-Nal)-FwLL-NH2 可用于肥胖研究。

K-(D-1-Nal)-FwLL-NH2amp;;

K-(D-1-Nal)-FwLL-NH2 Chemical Structure

CAS No. : 1394288-22-2

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

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生物活性

K-(D-1-Nal)-FwLL-NH2 is a high affinity, potent and inverse ghrelin receptor agonist (EC50=3.4 nM, Ki=4.9 nM). K-(D-1-Nal)-FwLL-NH2 can be used for the research of obesity[1].

IC50 Target

EC50: 3.4 nM (ghrelin receptor), Ki: 4.9 nM (ghrelin receptor)[1]
分子量

902.13

Formula

C51H67N9O6
CAS 号

1394288-22-2
Sequence Shortening

K{Nal}FWLL-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]. Els S, et al. An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor. J Med Chem. 2012;55(17):7437-7449.