奈他地尔 二甲磺酸盐
| CAS号 | 1422144-42-0 | 货号 | BCP24703 |
| 中文名 | 奈他地尔 二甲磺酸盐 | ||
| 英文名 | Netarsudil mesylate | ||
| 中文别名 | |||
| 英文别名 | AR-13324 mesylate;AR13324 mesylate;AR 13324 mesylate; | ||
| 分子式 | C30H35N3O9S2 | 分子量 | 645.74 |
| 生物活性 | Netarsudil, also known as AR-11324, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Netarsudil inhibited kinases ROCK1 and ROCK2 with a Ki of 1 nM each, disrupted actin stress fibers and focal adhesions in TM cells with IC50s of 79 and 16 nM, respectively, and blocked the profibrotic effects of TGF-β2 in HTM cells. Netarsudil produced large reductions in IOP in rabbits and monkeys that were sustained for at least 24 h after once daily dosing, with transient, mild hyperemia observed as the only adverse effect. | ||
| 信号通路 | Cell Cycle/DNA Damage TGF beta/Smad Wnt/Stem Cell | ||
| 靶 点 | ROCK | ||
结构式
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