Verosudil

Verosudil is an inhibitor of Rho-associated kinase 1 (ROCK1) and ROCK2 (K_i = 2 nM for both).¹ It is selective for ROCK1 and ROCK2 over PKA, PKCθ, Cdc42-binding kinase α (MRCKα), and calcium/calmodulin-dependent protein kinase IV (CaMKIV; K_is = 69, 9,332, 28, and 5,855 nM, respectively). Verosudil (1 µM) decreases focal adhesion points on, and actin fiber length in, primary porcine trabecular meshwork (PTM) cells. It inhibits TGF-β-induced increases in α-smooth muscle actin (α-SMA) levels in primary human conjunctival fibroblasts when used at concentrations of 250 or 500 nM.² Verosudil inhibits TGF-β-induced migration in a wound healing assay using primary human conjunctival fibroblasts. It reduces intraocular pressure (IOP) in rabbits and Formosan rock monkeys when ocularly administered at a concentration of 0.5%.¹ Ocular administration of verosudil (0.5%) decreases IOP and subconjunctival collagen levels in a rabbit model of trabeculectomy.²

WARNING This product is not for human or veterinary use.

1. Lin, C.W., Sherman, B., Moore, L.A., et al. Discovery and preclinical development of netarsudil, a novel ocular hypotensive agent for the treatment of glaucoma. J. Ocul. Pharmacol. Ther. 34(1-2), 40-51 (2018).

2. Cheng, W.S., Chen, C.L., Chen, J.T., et al. AR12286 alleviates TGF-β-related myofibroblast transdifferentiation and reduces fibrosis after glaucoma filtration surgery. Molecules 25(19), 4422 (2020).