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Ripasudil free base

产品编号 T7492 CAS 223645-67-8

别名: K-115 (free base)

Ripasudil free base (K-115 (free base)) 是一种ROCK 特异性抑制剂，能够抑制ROCK1和ROCK2的活性，IC50值分别为 51 和 19 nM。

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Ripasudil free base, CAS 223645-67-8

规格	价格/CNY	货期
1 mg	￥ 619	待询
5 mg	￥ 1,352	待询
10 mg	￥ 2,197	待询
25 mg	￥ 4,732	待询
50 mg	￥ 8,366	待询
100 mg	￥ 12,941	待询
1 mL * 10 mM (in DMSO)	￥ 1,177	待询

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Ripasudil free base 的其他形式现货产品:

Ripasudil

其他形式的 Ripasudil free base:

Ripasudil
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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Ripasudil free base (K-115 (free base)) is a selective and potent ROCK inhibitor, is a novel and potent antiglaucoma agent.
靶点活性	ROCK1:51 nM, ROCK2:19 nM, CaMK IIa:370 nM, PKC:27 μM, PKACa:2.1 μM
体外活性	Ripasudil significantly reduced infiltrating cells and protein exudation in the aqueous humor, as well as the number of infiltrating cells in the ICB and adherent leukocytes in retinal vessels in EIU. Additionally, the protein level of MCP-1 in the aqueous humor and mRNA levels of IL-1β, IL-6, TNF-α, MCP-1, and intercellular adhesion molecule-1 in the ICB and retina were suppressed by ripasudil. The production of MCP-1 and nuclear translocation of NF-κB in RAW264.7 cells were also suppressed by ripasudil[1].
体内活性	K-115 had selective and potent inhibitory effects on ROCKs.?In rabbits, topical instillation of K-115 significantly reduced IOP in a dose-dependent manner.?Maximum IOP reduction was observed 1 h after topical instillation, which was 8.55 ± 1.09 mmHg (mean ± SE) from the baseline IOP at 0.5%.?In monkeys, maximum IOP reduction was observed 2 h after topical instillation, which was 4.36 ± 0.32 mmHg from the baseline IOP at 0.4%, and was significantly stronger than that of 0.005% latanoprost.?Whole-head autoradiography showed that the radioactivity level was maximum at 15 min after instillation of [(14)C]K-115 in the ipsilateral eye.?Single instillation of 0.4% K-115 showed no effect on aqueous flow rate or uveoscleral outflow, but significantly increased conventional outflow facility by 2.2-fold compared to vehicle-treated eyes in rabbits[2].
细胞实验	Endotoxin-induced uveitis was induced by footpad injection of lipopolysaccharide (LPS). Ripasudil was administered intraperitoneally 1 hour before and after LPS injection. The aqueous humor was collected 24 hours after injection, and the infiltrating cells, protein concentration, and levels of monocyte chemotactic protein-1 (MCP-1) were determined. Infiltrating cells in the iris ciliary body (ICB) and adherent leukocytes in retinal vessels were evaluated. The mRNA levels of IL-1β, IL-6, TNF-α, and MCP-1 in the retina and ICB were determined. A mouse macrophage cell line, RAW264.7, was stimulated with LPS in the presence or absence of ripasudil, and the expression of MCP-1 and nuclear translocation of nuclear factor (NF)-κB was analyzed[1].
动物实验	Kinase inhibition by K-115 was measured by biochemical assay.?IOP was monitored using a pneumatonometer in albino rabbits and monkeys after topical instillation of K-115.?The ocular distribution of [(14)C]K-115 was determined by whole-head autoradiography.?The aqueous flow rate was determined by fluorophotometry.?The total outflow facility and uveoscleral outflow were measured by two-level constant pressure perfusion and perfusion technique using fluorescein isothiocyanate-dextran, respectively[2].

别名	K-115 (free base)
分子量	323.39
分子式	C15H18FN3O2S
CAS No.	223645-67-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Takatoshi U , Megumi H , Reiko Y , et al. The Anti-Inflammatory Effect of Ripasudil (K-115), a Rho Kinase (ROCK) Inhibitor, on Endotoxin-Induced Uveitis in Rats[J]. Investigative Opthalmology & Visual Science, 2017, 58(12):5584-. 2. Isobe T , Mizuno K , Kaneko Y , et al. Effects of K-115, a Rho-Kinase Inhibitor, on Aqueous Humor Dynamics in Rabbits[J]. Current Eye Research, 2014, 39(8):813-822.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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