|N-(4-甲氧基苄基)-1-(萘-1-基)甲胺盐酸盐|CsnPharm

CAS No.: 1222781-70-5

ML133 HCl/ML133 盐酸盐 Catalog No. CSN13712

Synonyms: ML-133 (hydrochloride)

ML133 HCl selectively inhibit Kir2.1 with IC50 of 1.8 μM at pH7.4 and 290 nM at pH8.5 and has no effect on Kir1.1 and weak activity for Kir4.1 and Kir7.1.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Potassium Channel Kir2.1

IC50:290nM(pH8.5)
描述ML133 hydrochloride is a selective Kir2 family channels inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5, but exhibits little selectivity against other members of Kir2.x family channels. ML133 has no effect on Kir1.1 (IC50 > 300 μM), and displays weak activity for Kir4.1 (76 μM) and Kir7.1 (33 μM), making ML133 the most selective small molecule inhibitor of the Kir family reported to date^[3]. Transplantation of ML133-treated or Kir2.1 knockdown EPCs (Endothelial progenitor cells) facilitated re-endothelialization in the rat injured arterial segment and inhibited neointima formation in vivo. In parallel, ML133 significantly enhanced autophagy and autophagic flux. After suppression of autophagy by 3-methyladenine (3-MA), the effects of ML133 on in vitro function and in vivo endothelialization capacity of EPCs were significantly inhibited^[4].
参考文献

[1] Lam D, Schlichter LC. Expression and contributions of the Kir2.1 inward-rectifier K(+) channel to proliferation, migration and chemotaxis of microglia in unstimulated and anti-inflammatory states. Front Cell Neurosci. 2015 May 12;9:185.
[2] Wang HR, Wu M, et al. Selective inhibition of the K(ir)2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR, and pharmacological characterization of ML133. ACS Chem Biol. 2011 Aug 19;6(8):845-56.
[3] Wang HR, Wu M, Yu H, et al. Selective inhibition of the K(ir)2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR, and pharmacological characterization of ML133. ACS Chem Biol. 2011;6(8):845-856
[4] Zhang X, Cui X, Li X, et al. Inhibition of Kir2.1 channel-induced depolarization promotes cell biological activity and differentiation by modulating autophagy in late endothelial progenitor cells. J Mol Cell Cardiol. 2019;127:57-66

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1865 mL
- 15.9326 mL
- 31.8653 mL
- 5 mM
- 0.6373 mL
- 3.1865 mL
- 6.3731 mL
- 10 mM
- 0.3187 mL
- 1.5933 mL
- 3.1865 mL

技术信息

CAS号

1222781-70-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H20ClNO

运输

蓝冰

分子量

313.82

别名

ML-133 (hydrochloride)

溶解度

DMSO	63.0 mg/mL (200.8 mM)
Water	Insoluble
Ethanol	6.0 mg/mL (19.1 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

ML133 HCl/ML133 盐酸盐 Catalog No. CSN13712

靶点选择性

请登录您的专属账户

确认信息