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Netarsudil(Mesylate) 编号 : 712181

化学信息

产品英文名称Netarsudil(Mesylate)
Iupac 化学名称(S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate dimethanesulfonate
同义词AR-13324; AR13324; AR 13324; Netarsudil Mesylate
英文同义词AR-13324; AR13324; AR 13324; Netarsudil Mesylate
分子式C30H35N3O9S2
分子量645.74
SmileCS(=O)(O)=O.CS(=O)(O)=O.O=C(OCC1=CC=C([C@@H](CN)C(NC2=CC3=C(C=NC=C3)C=C2)=O)C=C1)C4=CC=C(C)C=C4C
InChiKeyQQDRLKRHJOAQDC-FBHGDYMESA-N
InChiInChI=1S/C28H27N3O3.2CH4O3S/c1-18-3-10-25(19(2)13-18)28(33)34-17-20-4-6-21(7-5-20)26(15-29)27(32)31-24-9-8-23-16-30-12-11-22(23)14-24;2*1-5(2,3)4/h3-14,16,26H,15,17,29H2,1-2H3,(H,31,32);2*1H3,(H,2,3,4)/t26-;;/m1../s1
Cas1422144-42-0

技术数据

外观淡黄色至类白色固体
纯度HPLC>99%; Chiral HPLC EE>98%
可溶性可溶于DMSO
存储短期可在0-4度保存,数天至数月;长期可在-20度保存三年。
运输条件产品可以在室温下运输
质量控制 HNMR HPLC MS COA

产品详情

Netarsudil( 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.

结构

712181 - Netarsudil(Mesylate) | CAS 1422144-42-0

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