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ML133 HCl

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Chemical Structure| 1222781-70-5 同义名 : ML-133 (hydrochloride);ML133 hydrochloride
CAS号 : 1222781-70-5
货号 : A190932
分子式 : C19H20ClNO
纯度 : 97%
分子量 : 313.821
MDL号 : MFCD20921521
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(334.59 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Potassium Channel

    Kir2.1, IC50:290 nM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.19mL

0.64mL

0.32mL

15.93mL

3.19mL

1.59mL

31.87mL

6.37mL

3.19mL
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