| CAS NO: | 928320-12-1 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at RT |
| M.Wt | 333.38 |
| Cas No. | 928320-12-1 |
| Formula | C20H19N3O2 |
| Solubility | Soluble in DMSO |
| Chemical Name | (S,Z)-N'-(2-hydroxy-1-phenylethyl)-N-(4-(pyridin-4-yl)phenyl)carbamimidic acid |
| Canonical SMILES | OC[C@](/N=C(O)/NC1=CC=C(C2=CC=NC=C2)C=C1)([H])C3=CC=CC=C3 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
AS1892802是ROCK的强效选择性抑制剂,对人ROCK2\大鼠ROCK2和人ROCK1的IC50值分别为52\57和122 nM[1].
Rho激酶(ROCK)是一种丝氨酸-苏氨酸激酶,是小GTP结合蛋白Rho的下游效应子.ROCK磷酸化靶蛋白,例如肌球蛋白轻链激酶和LIM激酶,调节细胞形状改变\迁移\生长和收缩[2].
AS1892802是一种强效的ROCK抑制剂.AS1892802抑制ROCK1和ROCK2的IC50值分别为1.69和0.10 μM[3].在ATDC5细胞中,AS1892802诱导细胞分化.在HIG82细胞中,AS1892802显著抑制IL-1β或缓激肽诱导的前列腺素E2生成[4].
在免疫佐剂诱导的关节炎(AIA)大鼠模型和monoiodoacetate诱导的关节炎(MIA)大鼠模型中,AS1892802表现出强效的镇痛作用,ED50值为0.15 mg/kg[1].在monoiodoacetate诱导的关节炎和链脲佐菌素诱导的神经病模型中,AS1892802具有镇痛作用[2].在MIA注射的大鼠中,膝关节中ROCK I和II的mRNA表达水平增加.AS1892802以剂量依赖的方式显著抑制软骨损伤[4].
参考文献：
[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 Pharmaco
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