Epsilon-V1-2(Synonyms: ε-V1-2 EAVSLKPT)

Epsilon-V1-2;(Synonyms: ε-V1-2; EAVSLKPT) 纯度: 98.18%

Epsilon-V1-2 (ε-V1-2) 是一种 PKCε 衍生肽,是一种选择性 PKCε 抑制剂。Epsilon-V1-2 抑制 PKCε 的转运,但不抑制 α-,β- 和 δPKC 的转运。

Epsilon-V1-2amp;;(Synonyms: ε-V1-2;  EAVSLKPT)

Epsilon-V1-2 Chemical Structure

CAS No. : 182683-50-7

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10 mg ¥3200 In-stock
25 mg ¥6400 In-stock
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Epsilon-V1-2 相关产品

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生物活性

Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC[1].

IC50 Target

PKCε

;

体外研究
(In Vitro)

Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide containing the site for its specific receptor for activated C kinase (RACK), inhibits translocation of PKCε and reduces insulin response to glucose[1].
Epsilon-V1-2 (ε-V1-2; 1 µM, 24 hours) treatment significantly inhibits Oleic acid (OA)-induced connexin 43 (Cx43) Ser368 phosphorylation and prevents OA-induced gap junction disassembly in cardiomyocytes[2].

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

体内研究
(In Vivo)

Epsilon-V1-2 (20 mg/kg/day; osmotic pumps; daily; for 4 weeks) treatment significantly improves the beating score in a murine heterotopic transplantation model. Epsilon-V1-2 reduces infiltration of macrophages and T cells into the cardiac grafts, and decreases parenchymal fibrosis. Epsilon-V1-2 treatment almost abolishes the rise in pro-fibrotic cytokine, TGF-β and monocyte recruiting chemokine MCP-1 levels[3].

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

Animal Model: C57BL/6J mice transplanted the hearts of FVB mice[3]
Dosage: 20 mg/kg/day
Administration: 0.1 mL osmotic pumps implanted subcutaneously; daily; for 4 weeks
Result: Significantly improved the beating score throughout the treatment.

分子量

843.96

Formula

C37H65N9O13

CAS 号

182683-50-7

Sequence Shortening

EAVSLKPT

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 : 50 mg/mL (59.24 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1849 mL 5.9245 mL 11.8489 mL
5 mM 0.2370 mL 1.1849 mL 2.3698 mL
10 mM 0.1185 mL 0.5924 mL 1.1849 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]. M Yedovitzky, et al. Translocation inhibitors define specificity of protein kinase C isoenzymes in pancreatic beta-cells. J Biol Chem. 1997 Jan 17;272(3):1417-20.

    [2]. Yuahn-Sieh Huang, et al. Mechanism of oleic acid-induced gap junctional disassembly in rat cardiomyocytes. J Mol Cell Cardiol. 2004 Sep;37(3):755-66.

    [3]. Tomoyoshi Koyanagi, et al. Pharmacological inhibition of epsilon PKC suppresses chronic inflammation in murine cardiac transplantation model. J Mol Cell Cardiol. 2007 Oct;43(4):517-22.