Sovesudil (PHP-201) HCl is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor (antagonist) with IC50s of 3.7 and 2.3 nM for ROCK I and ROCK II, respectively. Sovesudil HCl reduces intraocular pressure without causing congestion.

Physicochemical Properties

Molecular Formula	C23H23CLFN3O3
Molecular Weight	443.9
CAS #	2984963-50-8
Related CAS #	Sovesudil;1333400-14-8
Appearance	Light brown to brown solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	ROCK-I 3.7 nM (IC50) ROCK-II 2.3 nM (IC50)
ln Vitro	Human trabecular meshwork (HTM) cells can exhibit changed cellular behavior when exposed to sovesudil(PHP-201)(1 μM; 60 min) hydrochloride[1].
ln Vivo	In ocular normotensive and acute hypertensive rabbits, sovesudil hydrochloride (0.1%, 0.3%, and 0.5%; male New Zealand White rabbits) significantly lowers Intraocular Pressure (IOP) without producing pronounced hyperemia[1].
References	[1]. 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]. 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.

Solubility Data

Solubility (In Vitro)

DMSO :~62.5 mg/mL (~140.80 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.69 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.2528 mL	11.2638 mL	22.5276 mL
	5 mM	0.4506 mL	2.2528 mL	4.5055 mL
	10 mM	0.2253 mL	1.1264 mL	2.2528 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.