SAR407899 hydrochloride is a selective, potent, and ATP-competitive ROCK inhibitor. It has an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. It inhibits ROCK-2 more effectively than ROCK-1. This product exhibits potent vasorelaxant activity in various isolated arteries and dose-dependently lowers blood pressure in hypertensive SHRs. It also increases penile length in healthy and diabetic rabbits.
- Selective and potent ROCK inhibitor
- ATP-competitive mechanism of action
- Inhibits MYPTT696 phosphorylation
- Blocks thrombin-induced effects
- Inhibits cell proliferation and migration
- Potent vasorelaxant activity
- Reduces blood pressure
- Increases penile length