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K-115
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。
K-115图片
CAS NO:887375-67-9
规格:98%
分子量:395.88
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
Selective Rho kinase inhibitor
CAS:887375-67-9
分子式:C15H23ClFN3O4S
分子量:395.88
纯度:98%
存储:Store at -20°C

Background:

Ripasudil (K-115) is a novel and potent Rho kinase inhibitor with intraocular pressure-lowering effect. Rho-kinase can be activated by the small GTP-binding protein Rho. Growing evidence has demonstrated that Rho/Rho-kinase pathway has been involved in a variety of cellular functions, such as actin cytoskeleton organization, vascular smooth muscle cell (VSMC) contraction, cell adhesion and motility, cytokinesis, and gene expressions. Dysfunctions of these may result in the pathogenesis of cardiovascular disease such as coronary artery spasm [1].


In vivo: In optic nerve crush (NC) C57BL/6 mice model, oral administration of K-115 (1 mg/kg/d) increased 34 ± 3% survival of RGCs after NC [2].


Clinical Trials: In the phase 1 clinical trials, 0.05%, 0.1%, 0.2%, 0.4%, and 0.8% concentrations of K-115 increased the intraocular pressure (IOP) of healthy male adult volunteers from -1.6 mm Hg for placebo to -3.4, -2.2, -2.6, -4.0, and -4.3 mm Hg when tested in 2 hours after instillation [3]. In the phase 2 randomized clinical study, in patients with primary open-angle glaucoma or ocular hypertension, K-115 treatment (twice daily for 8 weeks) dose-dependently lowered the IOP level [4].


参考文献:
[1].Shimokawa H, Takeshita A.? Rho-kinase is an important therapeutic target in cardiovascular medicine[J]. Arteriosclerosis, thrombosis, and vascular biology, 2005, 25(9): 1767-1775.
[2].Yamamoto K, Maruyama K, Himori N, et al.? The Novel Rho Kinase (ROCK) Inhibitor K-115: A New Candidate Drug for Neuroprotective Treatment in GlaucomaNovel Rho Kinase Inhibitor[J]. Investigative ophthalmology & visual science, 2014, 55(11): 7126-7136.
[3].Tanihara H, Inoue T, Yamamoto T, et al.? Phase 1 clinical trials of a selective Rho kinase inhibitor, K-115[J]. JAMA ophthalmology, 2013, 131(10): 1288-1295.
[4].Tanihara H, Inoue T, Yamamoto T, et al.? Phase 2 randomized clinical study of a Rho kinase inhibitor, K-115, in primary open-angle glaucoma and ocular hypertension[J]. American journal of ophthalmology, 2013, 156(4): 731-736. e2.