Y-27632 2HCL

产品编号: DC1028 Featured
Y-27632 2HCL
结构式
129830-38-2
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应用领域
Y-27632 dihydrochloride 是口服有效的, ATP 竞争性的 ROCK-I 和 ROCK-II 抑制剂,Ki 分别为 220 nM 和 300 nM。Y-27632 dihydrochloride 诱导凋亡 (apoptosis)。Y-27632 dihydrochloride 通过上皮-间充质过渡样调节引发人诱导多能干细胞 (hIPSCs) 选择性地分化为间胚层谱系。
Cas No.: 129830-38-2
名称: (1R,4r)-4-((R)-1-aminoethyl)-N-(pyridin-4-yl)cyclohexanecarboxamide dihydrochloride
别名: Y-27632, Y27632, Y 27632
SMILES: C[C@H](C1CCC(CC1)C(=O)NC2=CC=NC=C2)N.Cl.Cl
分子式: C14H21N3O.2HCl
分子量: 320.26
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
产品编号 产品名称 应用领域
DC1028 Y-27632 2HCL Y-27632 dihydrochloride 是口服有效的, ATP 竞争性的 ROCK-I 和 ROCK-II 抑制剂,Ki 分别为 220 nM 和 300 nM。Y-27632 dihydrochloride 诱导凋亡 (apoptosis)。Y-27632 dihydrochloride 通过上皮-间充质过渡样调节引发人诱导多能干细胞 (hIPSCs) 选择性地分化为间胚层谱系。