SAR407899

• CAT Number: I005493
• CAS Number: 923359-38-0
• Molecular Formula: C14H16N2O2
• Molecular Weight: 244.30
• Purity: ≥95%
• Synonyms: SAR-407899;SAR 407899
• Target: ROCK
• Solubility: DMSO: ≤ 6 mg/mL (Need warming)
• Storage: Store at -20°C
• IC50: 36 nM/41 nM(Ki, human/Rat ROCK)
• IUPAC Name: 6-piperidin-4-yloxy-2H-isoquinolin-1-one
• InChI: InChI=1S/C14H16N2O2/c17-14-13-2-1-12(9-10(13)3-8-16-14)18-11-4-6-15-7-5-11/h1-3,8-9,11,15H,4-7H2,(H,16,17)
• InChIKey: IPEXHQGMTHOKQV-UHFFFAOYSA-N
• SMILES: C1CNCCC1OC2=CC3=C(C=C2)C(=O)NC=C3

SAR407899 (Cat No.:I005493) is a potent and ATP-competitive inhibitor of Rho-associated protein kinase (ROCK). It exhibits a high binding affinity for both human ROCK (Ki value of 36 nM) and rat ROCK (Ki value of 41 nM). By selectively targeting ROCK, SAR407899 interferes with its kinase activity, which plays a crucial role in various cellular processes. This compound’s ability to modulate ROCK activity makes it a valuable tool for investigating the functions and pathways influenced by ROCK, potentially contributing to advancements in understanding and treating related physiological and pathological conditions.

Reference

[1]. Lohn M, et al. Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor. Hypertension. 2009 Sep;54(3):676-83. 


[2]. Grisk O, et al. The Rho kinase inhibitor SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. J Hypertens. 2012 May;30(5):980-9. 


[3]. Guagnini F, et al. Erectile properties of the Rho-kinase inhibitor SAR407899 in diabetic animals and human isolated corpora cavernosa. J Transl Med. 2012 Mar 23;10:59.