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CAS:129830-38-2
品牌:MedChemExpress (MCE)
存储条件:4°C, sealed storage, away from moisture
生物活性:Y-27632 dihydrochloride 是一种具有口服活性和 ATP 竞争性的 ROCK (Rho-kinase) 抑制剂 (ROCK-I Ki /b>=220nM;ROCK-II Ki=300 nM)。 Y-27632 dihydrochloride 具有抗癫痫作用[1][2][3][4]。 IC50 和目标:Ki:220/300 nM (ROCK-I/II)[1]
体外:Y-27632(1-5 μM;0-60 分钟)促进脂肪组织来源的干细胞 (ADSCs) 的神经元分化[3]。Y-27632 (1-5 μM ; 0-60 分钟) 诱导 ADSCs 中 NSE、MAP-2 和巢蛋白的表达 [3]。
体内:Y-27632(口服灌胃;30 mg/kg;每日一次;4 周)预防二甲基亚硝胺诱导的大鼠肝纤维化[1]。Y-27632(口服灌胃;5- 10 mg/kg; once) 对 PTZ 和 MES 诱发的癫痫有抗癫痫作用[2]。
参考文献:
[1]. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36.
[2]. Inan S, et al. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. Br J Pharmacol. 2008 Sep;155(1):44-51.
[3]. Xue ZW, et al. Rho-associated coiled kinase inhibitor Y-27632 promotes neuronal-like differentiation of adult human adipose tissue-derived stem cells. Chin Med J (Engl). 2012 Sep;125(18):3332-5.
[4]. Ishizaki T, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.
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