| Bioactivity | Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil lowers intraocular pressure (IOP) without inducing hyperemia[1][2]. | ||||||||||||
| Invitro | Sovesudil (PHP-201) (1 μM; 60 min) is able to induce altered cellular behavior of human trabecular meshwork (HTM) cells[1]. | ||||||||||||
| 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[1]. | ||||||||||||
| Name | Sovesudil | ||||||||||||
| CAS | 1333400-14-8 | ||||||||||||
| Formula | C23H22FN3O3 | ||||||||||||
| Molar Mass | 407.44 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |