Ripasudil (Synonyms: K-115)
目录号: PL11042 纯度: ≥98%
CAS No. :887375-67-9
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中文名称
Ripasudil
中文别名
(2S)-1-[(4-氟-5-异喹啉基)磺酰基]六氢-2-甲基-1H-1,4-二氮杂卓单盐酸盐二水合物;(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
英文名称
Ripasudil
英文别名
K115;K-115 Hydrochloride Dihydrate;Ripasudil;K-115;Ripasudil hydrochloride dihydrate;016TTR32QF;Ripasudil hydrochloride hydrate [JAN];Ripasudil hydrochloride hydrate (JAN);Ripasudil hydrochloride hydrate;Glanatec (TN);Ripasudil hydrochloride dihydrate [WHO-DD];C15H18FN3O2S.ClH.2H2O;BCP11082;s7995;3757AH;1H-1,4-Diazepine, 1-((4-fluoro-5-is;1H-1,4-Diazepine, 1-[(4-fluoro-5-isoquinolinyl)sulfonyl]hexahydro-2-methyl-, monohydrochloride, dihydrate, (2S)- (9CI);Ripasudil monohydrochloride dihydrate
Cas No.
887375-67-9
分子式
C15H21ClFN3O3S
分子量
377.86
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Ripasudil (K-115) 是 ROCK 特异性抑制剂,能够抑制 ROCK2 和 ROCK1 的活性,IC50 值分别为 19 和 51 nM。
生物活性
Ripasudil (K-115) is a specific inhibitor of ROCK, with IC 50 s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
性状
Solid
IC50 & Target[1][2]
ROCK2 19 nM (IC50) ROCK1 51 nM (IC50
体外研究(In Vitro)
Ripasudil (K-115) is a potent inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively. Ripasudil also shows less potent inhibitory activities against CaMKIIα, PKACα and PKC, with IC50s of 370 nM, 2.1 μM and 27 μM, respectively. Ripasudil (K-115; 1, 10 μM) induces cytoskeletal changes, including retraction and cell rounding and reduced actin bundles of cultured trabecular meshwork (TM) cells. Ripasudil (5 μM) sifnificantly reduces transendothelial electrical resistance (TEER), and increases FITC-dextran permeability in Schlemm’s canal endothelial (SCE) cell monolayers. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Ripasudil (K-115) reduces intraocular pressure (IOP) in a concentration-dependent manner at concentrations between 0.1% and 0.4% in monkey eyes and 0.0625% to 0.5% in rabbit eyes, respectively. Ripasudil (K-115; 1 mg/kg, p.o. daily) shows a neuroprotective effect on retinal ganglion cells (RGCs) after nerve crush (NC). Ripasudil also inhibits the oxidative stress induced by axonal injury in mice. Ripasudil suppresses the time-dependent production of ROS in RGCs after NC injury. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
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 Schlemms canal endothelial cells. Sci Rep. 2016 Jan 19;6:19640.
溶解度数据
In Vitro: H2O : ≥ 50 mg/mL (126.30 mM)DMSO : 25 mg/mL (63.15 mM; Need ultrasonic)
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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