FREE BASE CASE;PNWBYIFLWUCWKS-UHFFFAOYSA-N;Reaxys ID: 21768535;[1,1'-Biphenyl]-3-carboxylic acid, 2'-(aminomethyl)-5'-[[(3-fluoro-4-pyridinyl)amino]carbonyl]-, propyl ester;Sovesudil;AMA0076);Sovesudil (PHP-201
Cas No.
1333400-14-8
分子式
C23H22FN3O3
分子量
407.44
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Sovesudil (PHP-201) 是一种有效的、ATP 竞争性局部作用 Rho激酶 (ROCK) 抑制剂,对 ROCK I 和 ROCK II 的 IC50 分别为 3.7 和 2.3 nM。Sovesudil 降低眼压而不引起充血。
生物活性
Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC 50 s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil lowers intraocular pressure (IOP) without inducing hyperemia.
性状
Solid
IC50 & Target[1][2]
ROCK-I 3.7 nM (IC50) ROCK-II 2.3 nM (IC
体外研究(In Vitro)
Sovesudil (PHP-201) (1 μM; 60 min) is able to induce altered cellular behavior of human trabecular meshwork (HTM) cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Sovesudil (0.1%, 0.3%, and 0.5%; male New Zealand White rabbits) effectively reduces Intraocular Pressure (IOP) in ocular normotensive and acute hypertensive rabbits without causing distinct hyperemia. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Van de Velde S, et al. AMA0076, a novel, locally acting Rho kinase inhibitor, potently lowers intraocular pressure in New Zealand white rabbits with minimal hyperemia. Invest Ophthalmol Vis Sci. 2014;55(2):1006-1016. Published 2014 Feb 18. [2]. Ha A, et al. Sovesudil (locally acting rho kinase inhibitor) for the treatment of normal-tension glaucoma: the randomized phase II study [published online ahead of print, 2021 Jul 28]. Acta Ophthalmol. 2021;10.1111/aos.14949.
溶解度数据
In Vitro: DMSO : 100 mg/mL (245.43 mM; Need ultrasonic)配制储备液