aladdin 阿拉丁 R413902 二水合物利帕西地尔（K-115）盐酸盐 887375-67-9 99%

中文名：二水合物利帕西地尔（K-115）盐酸盐

英文名：Ripasudil (K-115) hydrochloride dihydrate

纯度：≥99%

货号：R413902

Cas号：887375-67-9

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

Ripasudil (K-115) hydrochloride dihydrate is potentROCKinhibitor withIC50of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.

Targets

ROCK2 (Cell-free assay); ROCK1 (Cell-free assay) 19 nM; 51 nM

In vitro

In monkey trabecular meshwork (TM) cells, Ripasudil induces retraction and rounding of cell bodies as well as disruption of actin bundles. In Schlemm\'s canal endothelial (SCE) cells, Ripasudil significantly decreases transendothelial electrical resistance (TEER), increases the transendothelial flux of FITC-dextran, and disrupts cellular localization of ZO-1 expression.

In vivo

In albino rabbits and monkeys, topical instillation of Ripasudil significantly reduces intraocular pressure (IOP) with maximum IOP reduction of 8.55 mmHg and 4.36 mmHg at 0.5 % and 0.4%, respectively. Ripasudil (1 mg/kg daily, p.o.) exerts a neuroprotective effect on retinal ganglion cell (RGC) after optic nerve crush (NC) by suppressing oxidative stress through pathways involving the Nox family in a mouse model.

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