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Netarsudil CAS# 1254032-66-0 奈他地尔游离碱

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.
📌 参考资料/链接:
Reference: Sturdivant, Jill M.; Delong, Mitchell A.; Chambournier, Gilles; Pamment, Michael G.; Fedij, Victor. Process for the preparation of kinase inhibitors and intermediates thereof. WO 2017086941. (Assignee Aerie Pharmaceuticals, Inc., USA)

📄 详细内容

CAS No. 1254032-66-0 奈他地尔游离碱Netarsudil synthetic routes


Sturdivant, Jill M.; Delong, Mitchell A.; Chambournier, Gilles; Pamment, Michael G.; Fedij, Victor. Process for the preparation of kinase inhibitors and intermediates thereof. WO 2017086941. (Assignee Aerie Pharmaceuticals, Inc., USA)
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