| Identification | Back Directory | [Name]
FREE BASE CASE | [CAS]
1333400-14-8 | [Synonyms]
AMA0076)
Sovesudil
FREE BASE CASE
Reaxys ID: 21768535
Sovesudil (PHP-201
PNWBYIFLWUCWKS-UHFFFAOYSA-N
[1,1'-Biphenyl]-3-carboxylic acid, 2'-(aminomethyl)-5'-[[(3-fluoro-4-pyridinyl)amino]carbonyl]-, propyl ester | [Molecular Formula]
C23H22FN3O3 | [MOL File]
1333400-14-8.mol | [Molecular Weight]
407.44 |
| Chemical Properties | Back Directory | [Boiling point ]
545.9±50.0 °C(Predicted) | [density ]
1.265±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (245.43 mM; Need ultrasonic) | [form ]
Solid | [pka]
8.84±0.70(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | [IC 50]
ROCK-I: 3.7 nM (IC50); ROCK-II: 2.3 nM (IC50) | [References]
[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. DOI:10.1167/iovs.13-13157
[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. DOI:10.1111/aos.14949 |
|
|