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Please store the product under the recommended conditions in the Certificate of Analysis.
- 英文名：
K-115 (free base)
- 库存：
货期：电询
- 供应商：
MedChemExpress LLC
- CAS号：
223645-67-8
- 规格：
电询
MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。
Ripasudil free base
CAS No. : 223645-67-8
MCE 国际站：Ripasudil free base
产品活性：Ripasudil free base (K-115 free base) 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。
研究领域：Cell Cycle/DNA Damage | Stem Cell/Wnt | Cytoskeleton | TGF-beta/Smad
作用靶点：ROCK
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.
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.
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