|(S)-4-氟-5-((2-甲基-1,4-二氮杂卓-1-基)磺酰基)异喹啉盐酸盐二水合物|CsnPharm

CAS No.: 887375-67-9

(S)-4-Fluoro-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline hydrochloride dihydrate Catalog No. CSN16952

Synonyms: K-115;K 155;brand name: Glanatec

K-115 HCl is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 ROCK2

IC50:19nM ROCK1

IC50:51nM
描述Ripasudil (K-115), a fluorinated analog of fasudil, is a ROCK inhibitor used for the treatment of glaucoma, with IC50 values of 51nM and 19nM for ROCK1 and ROCK2, also with IC50s 111, 1420, and 19.5 times higher than that for ROCK 2 for PKACα, PKC, and CaMKIIα. Administration of Ripasudil at concentration of 0.0625%, 0.125%, 0.25% and 0.5% dose-dependently decreased intraocular pressure in rabbit eyes within 1h. Also, monkey eyes dosed of 0.1%, 0.2% and 0.4% showed dose-dependent maximum IOP reduction. Treatment with 0.4% Ripasudil increased outflow facility to 2.2 fold compared with control in rabbits. Intravitreal injection with 200pM Ripasudil for 2 weeks diminished p62 and enhanced LC3-II protein levels significantly compared with both baseline and TNF-induced group of rat optic nerves, suggesting a ripasudil-enhanced intra-axonal autophagy. Intraperitoneal injection with 0.1 mL of ripasudil (20 mg/ml) 1 hour before and after LPS injection in male rats showed a potent anti-inflammatory effect against ocular inflammatory diseases. LPS-induced infiltrating cell number, MCP-1 in aqueous humor, retinal leukocyte adhesion, as well as mRNA levels of proinflammatory mediators, including IL-1β, IL-6, TNF-α, MCP-1 and ICAM-1, in both retina and iris-ciliary body could be inhibited after ripasudil treatment. 100μM treatment with ripasudil could also inhibited MCP-1 and nuclear translocation of NF-κB induced by LPS in RAW 264.7 cells.
动物研究
剂量
Mice: 1 mg/kg/d^[2] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 1 mg/kg/d^[2] (p.o.)
给药途径	p.o.

[1] Kaneko Y, Ohta M, et al. Effects of K-115 (Ripasudil), a novel ROCK inhibitor, on trabecular meshwork and Schlemm's canal endothelial cells. Sci Rep. 2016 Jan 19;6:19640.
[2] Yamamoto K, Maruyama K, et al. The novel Rho kinase (ROCK) inhibitor K-115: a new candidate drug for neuroprotective treatment in glaucoma. Invest Ophthalmol Vis Sci. 2014 Oct 2;55(11):7126-36.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5260 mL
- 12.6302 mL
- 25.2604 mL
- 5 mM
- 0.5052 mL
- 2.5260 mL
- 5.0521 mL
- 10 mM
- 0.2526 mL
- 1.2630 mL
- 2.5260 mL

技术信息

CAS号

887375-67-9

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H23ClFN3O4S

运输

蓝冰

分子量

395.88

别名

K-115;K 155;brand name: Glanatec

溶解度

DMSO	25.0 mg/mL (63.2 mM) warming
Ethanol	5.0 mg/mL (12.6 mM) warming

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

靶点	Description	IC50
ROCK2		IC50:19nM
ROCK1		IC50:51nM

(S)-4-Fluoro-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline hydrochloride dihydrate Catalog No. CSN16952

靶点选择性

请登录您的专属账户

确认信息