Y-27632 2HCL 产品说明书 Chemicals
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产品编号 DC1028
名称 Y-27632 2HCL

化学性质

CAS 129830-38-2
分子式 C14H21N3O.2HCL
分子量 320.26
存储条件 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

生物活性

Description CAS NO.:12983-38-2
Product Name:(1R,4r)-4-((R)-1-aminoethyl)-N-(pyridin-4-yl)cyclohexanecarboxamide dihydrochloride
Synonyms:Y-27632, Y27632, Y 27632
EINEC:
Molecular Formula:C14H21N3O.2HCl
Molecular Weight:32.26
In Vivo
In Vitro

化合物的使用

Kinase Assay
Cell Assay
Animal Administration

参考文献


Y-27632 2Hcl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK. IC50 value: 140 nM (Ki) Target: ROCK1 in vitro: Y-27632 inhibits ROCK-II while displaying little activity against PKC, cAMP-dependent protein kinase and myosin light-chain kinase (MLCK) with Ki of 26 μM, 25 μM and > 250 μM, respectively, as well as PKA activated by another Rho-family GTPase member, Cdc42. Y-27632 inhibits smooth-muscle contraction induces by various agonists including phenylephrine, histamine, acetylcholine, serotonin, endothelin, and thromboxane with IC50 of 0.3-1 μM, by selectively inhibiting Ca2+ sensitization. Y-27632 suppresses Rho-induced, p160ROCK-mediated formation of stress fibres in cultured cells. In human embryonic stem (hES) cells, Y-27632 treatment at 10 μM markedly diminishes dissociation-induced apoptosis even in serum-free suspension (SFEB) culture, increases cloning efficiency (from ~1% to ~27%), facilitates subcloning after gene transfer, and enables SFEB-cultured hES cells to survive and differentiate into Bf1+ cortical and basal telencephalic progenitors. in vivo: Oral administration of Y-27632 at 30 mg/kg significantly decreases the blood pressure in a dose-dependent manner in spontaneous hypertensive rats, renal hypertensive rats, as well as deoxycorticosterone acetate (DOCA)-salt hypertensive rats. When Y-27632 is continuously administered at a rate of 0.55 μL per hour by implanted pumps for 11 days tumor cell invasion (MM1 cells expressing Val14-RhoA in rats) is significantly delayed. By inhibiting ROCK, Y-27632 treatment attenuates hypoxia-induced angiogenesis and vascular remodeling in the pulmonary circulation. For the detailed information about the solubility of Y-27632 2HCL in water, the solubility of Y-27632 2HCL in DMSO, the solubility of Y-27632 2HCL in PBS buffer, the animal experiment(test) of Y-27632 2HCL,the in vivo,in vitro and clinical trial test of Y-27632 2HCL,the cell experiment(test) of Y-27632 2HCL,the IC50, EC50 and Affinity of Y-27632 2HCL, please contact DC Chemicals.
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