生物活性

Y-27632 dihydrochloride is a selective Rho-kinase inhibitor, which suppresses cholinergic nerve-mediated contractions. Selective p160ROCK inhibitor (Ki values are 0.14, 26, 25 and > 250 μM for p160ROCK, PKC, PKA and MLCK respectively). Also inhibits PRK2 (IC50 = 600 nM). In addition, studies show that Y-27632 dihydrochloride increases the release of neurotransmitters from cholinergic nerves. Studies conducted on smooth muscle preparations suggest that Y-27632 dihydrochloride suppresses nerve-mediated contractile responses stimulated by acetylcholine and noradrenaline.

体外研究

体内研究

Saline

激酶实验

细胞实验

10 Μm

动物实验

30 mg/kg/day (Rat); 0-10 mg/kg (mice) Orally (Rat); i.p. (Mice)

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Uehata M, et al. Nature, 1997, 389(6654), 990-994.
[2] Davies, S P., et al., 2000. Specificity and mechanism of action of some commonly used protein kinase inhibitors. The Biochemical journal. 351(Pt 1): 95-105.
[3] Köksel, Oğuz., et al., 2005. Rho-kinase (ROCK-1 and ROCK-2) upregulation in oleic acid-induced lung injury and its restoration by Y-27632. European journal of pharmacology. 510(1-2): 135-42.
[4] Fernandes, Lynette., et al., 2006. A Rho-kinase inhibitor, Y-27632, reduces cholinergic contraction but not neurotransmitter release. European journal of pharmacology. 550(1-3): 155-61.
[5] Narumiya, S., et al., 2000. Use and properties of ROCK-specific inhibitor Y-27632. Methods in enzymology. 325(): 273-84.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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