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Ripasudil

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Chemical Structure| 887375-67-9 同义名 : K-115;K-115 Hydrochloride Dihydrate;Ripasudil hydrochloride dihydrate
CAS号 : 887375-67-9
货号 : A130094
分子式 : C15H23ClFN3O4S
纯度 : 99%+
分子量 : 395.877
MDL号 : MFCD26960897
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(63.15 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(126.3 mM)
动物实验配方：
生物活性
靶点

  • ROCK1

    ROCK1, IC50:51 nM

  • ROCK2

    ROCK2, IC50:19 nM
描述 Ripasudil (K-115) is a potent inhibitor of ROCK, with IC50 values of 19 nM and 51 nM for ROCK2 and ROCK1, respectively. It also demonstrates less potent inhibitory activity against CaMKIIα, PKACα, and PKC, with IC50 values of 370 nM, 2.1 μM, and 27 μM, respectively[1]. At concentrations of 1 and 10 μM, Ripasudil (K-115) induces cytoskeletal changes in cultured trabecular meshwork (TM) cells, including retraction and cell rounding, as well as reduced actin bundles. Additionally, at a concentration of 5 μM, it significantly reduces transendothelial electrical resistance (TEER) and increases FITC-dextran permeability in Schlemm’s canal endothelial (SCE) cell monolayers[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.63mL

2.53mL

1.26mL

25.26mL

5.05mL

2.53mL
参考文献

[1]Isobe T, et al. Effects of K-115, a rho-kinase inhibitor, on aqueous humor dynamics in rabbits. Curr Eye Res. 2014 Aug;39(8):813-22.

[2]Kaneko Y, 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.

[3]Yamamoto 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.