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AS 1892802
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AS 1892802图片
CAS NO:928320-12-1
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
AS 1892802 是一种有效的、具有口服活性的、高选择性的 ROCK 抑制剂。
Cas No.928320-12-1
化学名(S,Z)-N'-(2-hydroxy-1-phenylethyl)-N-(4-(pyridin-4-yl)phenyl)carbamimidic acid
Canonical SMILESOC[C@](/N=C(O)/NC1=CC=C(C2=CC=NC=C2)C=C1)([H])C3=CC=CC=C3
分子式C20H19N3O2
分子量333.38
溶解度DMF: 25 mg/ml,DMSO: 25 mg/ml,DMSO:PBS (pH 7.2) (1:7): 0.12 mg/ml
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AS 1892802 is a potent and selective inhibitor of ROCK with IC50 values of 52, 57 and 122 nM for human ROCK2, rat ROCK2 and human ROCK1, respectively [1].

Rho kinase (ROCK) is a serine-threonine kinase and is a downstream effector of Rho, a small GTP-bound protein. ROCK phosphorylates target proteins such as myosin light chain kinase and LIM kinase and regulates cellular shape modification, migration, growth and contraction [2].

AS 1892802 is a potent ROCK inhibitor. AS 1892802 inhibited ROCK1 and ROCK2 with IC50 values of 1.69 and 0.10 μM, respectively [3]. In ATDC5 cells, AS1892802 induce chondrocyte differentiation. In HIG82 cells, AS1892802 significantly inhibited prostaglandin E2 production induced by IL-1β or bradykinin [4].

In both an adjuvant-induced arthritis (AIA) rat model and a monoiodoacetate (MIA) -induced arthritis (MIA) rat model, AS1892802 showed potent antinociceptive effect with ED50 value of 0.15 mg/kg [1]. In monoiodoacetate-induced arthritis and streptozotocin-induced neuropathy models, AS1892802 showed analgesic effect [2]. In MIA-injected rats, the mRNA levels of ROCK I and II increased in knee joints. AS1892802 significantly inhibited cartilage damage in a dose-dependent way [4].

References:
[1].  Yoshimi E, Kumakura F, Hatori C, et al. Antinociceptive effects of AS1892802, a novel Rho kinase inhibitor, in rat models of inflammatory and noninflammatory arthritis. J Pharmacol Exp Ther, 2010, 334(3): 955-963.
[2].  Yoshimi E, Yamamoto H, Furuichi Y, et al. Sustained analgesic effect of the Rho kinase inhibitor AS1892802 in rat models of chronic pain. J Pharmacol Sci, 2010, 114(1): 119-122.
[3].  Li R, Martin MP, Liu Y, et al. Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors. J Med Chem, 2012, 55(5): 2474-2478.
[4].  Takeshita N, Yoshimi E, Hatori C, et al. Alleviating effects of AS1892802, a Rho kinase inhibitor, on osteoarthritic disorders in rodents. J Pharmacol Sci, 2011, 115(4): 481-489.