目錄:愛(ài)必信(上海)生物科技有限公司>>生化試劑>>小分子化合物>> abs810640Y-27632 2HCl
| 參考價(jià) | 445 |
參考價(jià):¥ 445
5mg
CAS:129830-38-2 純度:>98% 分子量:320.26 分子式:C14H21N3O.2HCl 供貨周期:現(xiàn)貨 規(guī)格:5mg 貨號(hào):abs810640 應(yīng)用領(lǐng)域:化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 主要用途:Y-27632 2HCl is a selective ROCK1 (p160R
>| 5mg | 445元 | 999mg可售 |
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| CAS | 129830-38-2 | 純度 | >98% |
|---|---|---|---|
| 分子量 | 320.26 | 分子式 | C14H21N3O.2HCl |
| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 5mg |
| 貨號(hào) | abs810640 | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
| 主要用途 | Y-27632 2HCl is a selective ROCK1 (p160R |
| 產(chǎn)品描述 | |
| 描述 | Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM. |
| 純度 | >98% |
| 儲(chǔ)存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | Y27632 dihydrochloride |
| 外觀 | white to beige powder |
| 可溶性/溶解性 | DMSO :64 mg/mL warmed (199.83 mM) Water :14 mg/mL (43.71 mM) |
| 生物活性 | |
| 靶點(diǎn) | ROCK1 (p160ROCK);ROCK2 |
| In vitro(體外研究) | Y-27632 2HCl 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 2HCl inhibits smooth-muscle contraction induces by various agonists including histamine, acetylcholine, serotonin, endothelin, and thromboxane with IC50 of 0.3-1 μM, by selectively inhibiting Ca2+ sensitization. Y-27632 2HCl suppresses Rho-induced, p160ROCK-mediated formation of stress fibres in cultured cells. Y-27632 2HCl treatment blocks both Rho-mediated activation of actomyosin and LPA-stimulated invasive activity of MM1 cells in a concentration-dependent manner. Y-27632 2HCl treatment is not only sufficient to initiate formation of exuberant axonal processes but also facilitates axonal maturation during the very early stages of axonogenesis, while largely sparing axon elongation. In human embryonic stem (hES) cells, Y-27632 2HCl 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(體內(nèi)研究) | Oral administration of Y-27632 2HCl 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 2HCl 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 2HCl treatment attenuates hypoxia-induced angiogenesis and vascular remodeling in the pulmonary circulation. Pretreatment with Y-27632 has a protective effect against tumor formation in albino mice with Ehrlich ascites carcinoma. |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | Stem CellsSignaling Pathways Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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