Verosudil

A ROCK1 and ROCK2 inhibitor (Ki = 2 nM for both), selective for ROCK1 and ROCK2 over PKA, PKCtheta, MRCKalpha, and CaMKIV (Kis = 69, 9,332, 28, and 5,855 nM, respectively), decreases focal adhesion points on, and actin fiber length in, primary PTM cells at 1 µM, inhibits TGF-beta-induced increases in alpha-SMA levels in primary human conjunctival fibroblasts at 250 or 500 nM, inhibits TGF-beta-induced migration in a wound healing assay using primary human conjunctival fibroblasts, reduces IOP in rabbits and Formosan rock monkeys when ocularly administered at 0.5%, decreases IOP and subconjunctival collagen levels in a rabbit model of trabeculectomy when ocularly administered at 0.5%. Formulation: A solid. InChI: InChI=1S/C17H17N3O2S/c1-20(2)15(12-6-8-23-10-12)17(22)19-13-3-4-14-11(9-13)5-7-18-16(14)21/h3-10,15H,1-2H3,(H,18,21)(H,19,22). InChIKey: VDYRZXYYQMMFJW-UHFFFAOYSA-N. SMILES: O=C1NC=CC2=C1C=CC(NC(C(C3=CSC=C3)N(C)C)=O)=C2