SAR407899 hydrochloride
CAS No. | 923262-96-8 | Cat. No. | BCP13153 |
Name | SAR407899 hydrochloride | ||
Synonyms | SAR-407899 hydrochloride;SAR 407899 hydrochloride; | ||
Formula | C14H17ClN2O2 | M. Wt | 280.75 |
Description | in vitro: SAR407899 is highly selective in panel of 117 receptor and enzyme targets. SAR407899 is ≈8-fold more active than fasudil. In vitro, SAR407899 demonstrated concentration-dependent inhibition of Rho-kinase–mediated phosphorylation of myosin phosphatase, thrombin-induced stress fiber formation, platelet-derived growth factor–induced proliferation, and monocyte chemotactic protein-1–stimulated chemotaxis. SAR407899 potently (mean IC50 values: 122 to 280 nM) and species-independently relaxed precontracted isolated arteries of different species and different vascular beds [1]. SAR407899 dose-dependently relaxed the pre-contracted corpora cavernosa in all species, with similar potency and efficacy in healthy vs diabetic rats, WKY vs SHR rats, healthy vs diabetic rabbits (IC(50) range from 0.05 to 0.29 μM, Emax range 89 to 97%) . in vivo: Over the dose range 3 to 30 mg/kg PO, SAR407899 lowered blood pressure in a variety of rodent models of arterial hypertension . SAR407899 was more | ||
Pathways | Cell Cycle/DNA Damage TGF beta/Smad Wnt/Stem Cell | ||
Targets | ROCK |
Structure
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