Verosudil

Verosudil (AR-12286) is a ROCK inhibitor. Verosudil has equal inhibitory activity against ROCK1 and ROCK2 (K_i: 2 nM). Verosudil is less selective for PKA, PKCT, MRCKA, and CAM2A (K_i: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil increases trabecular outflow capacity to reduce intraocular pressure. Verosudil is useful in the study of glaucoma and ocular hypertension^[1][2]. In Vitro:Verosudil (AR-12286) has significant inhibitory activity against both ROCK1 and ROCK2 (K_i: 2 nM)^[1].
Verosudil (0.001-100 μM, 6 hours) dose-dependently reduces the length of actin stress fibers in porcine primary trabecular meshwork cells (PTM)^[1].
Verosudil (0.001-100 μM, 6 hours) reduces the number of focal adhesions in immortalized human trabecular meshwork (HTM) cells^[1].
Verosudil has the ability to disrupt actin stress fibers and focal adhesions in PTM cells and HTM cells (IC₅₀: 924 nM and IC₅₀: 818 nM, respectively)^[1].
In Vivo:Verosudil (AR-12286) (30 μL, eye drops, once daily for 3 days) significantly reduces intraocular pressure in Dutch rabbits and Formosan rock monkeys^[1].
Verosudil (10 μL, eye drops, twice daily for five weeks) can reverse the changes in intraocular pressure, trabecular meshwork effective filtration area and morphology in a mouse model of ocular hypertension induced by Dexamethasone (HY-14648) ^[2].