4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Sovesudil (PHP-201) hydrochloride 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 hydrochloride 可降低眼压而不引起充血。
生物活性
Sovesudil (PHP-201) hydrochloride 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 hydrochloride 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) hydrochloride 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) hydrochloride 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
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 : 62.5 mg/mL (140.80 mM; ultrasonic and warming and heat to 60°C)配制储备液