WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 526770
CAS#: 923359-38-0 (free base)
Description: SAR407899 is a potent and selective Rho kinase inhibitor with promising antihypertensive activity. SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. SAR407899 is equipotent against human and rat-derived Rho-kinase 2 with inhibition constant values of 36 nM and 41 nM, respectively. SAR407899 is approximately 8-fold more active than fasudil. SAR407899 potently (mean IC(50) values: 122 to 280 nM) and species-independently relaxed precontracted isolated arteries of different species and different vascular beds. The antihypertensive effect of SAR407899 was superior to that of fasudil and Y-27632.
MedKoo Cat#: 526770
Name: SAR407899 free base
CAS#: 923359-38-0 (free base)
Chemical Formula: C14H16N2O2
Exact Mass: 244.1212
Molecular Weight: 244.294
Elemental Analysis: C, 68.83; H, 6.60; N, 11.47; O, 13.10
Related CAS #: 923262-96-8 (HCl) 923359-38-0 (free base)
Synonym: SAR407899; SAR 407899; SAR-407899; SAR407899 HCl
IUPAC/Chemical Name: 6-(piperidin-4-yloxy)isoquinolin-1(2H)-one
InChi Key: IPEXHQGMTHOKQV-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C1NC=CC2=C1C=CC(OC3CCNCC3)=C2
Related CAS#
CAS#923262-96-8 (HCl);
CAS#923359-38-0 (free base).
1: Löhn M, Plettenburg O, Kannt A, Kohlmann M, Hofmeister A, Kadereit D, Monecke P, Schiffer A, Schulte A, Ruetten H, Ivashchenko Y. End-organ protection in hypertension by the novel and selective Rho-kinase inhibitor, SAR407899. World J Cardiol. 2015 Jan 26;7(1):31-42. doi: 10.4330/wjc.v7.i1.31. PubMed PMID: 25632317; PubMed Central PMCID: PMC4306204.
2: Babelova A, Jansen F, Sander K, Löhn M, Schäfer L, Fork C, Ruetten H, Plettenburg O, Stark H, Daniel C, Amann K, Pavenstädt H, Jung O, Brandes RP. Activation of Rac-1 and RhoA contributes to podocyte injury in chronic kidney disease. PLoS One. 2013 Nov 7;8(11):e80328. doi: 10.1371/journal.pone.0080328. eCollection 2013. PubMed PMID: 24244677; PubMed Central PMCID: PMC3820652.
3: Guagnini F, Ferazzini M, Grasso M, Blanco S, Croci T. Erectile properties of the Rho-kinase inhibitor SAR407899 in diabetic animals and human isolated corpora cavernosa. J Transl Med. 2012 Mar 23;10:59. doi: 10.1186/1479-5876-10-59. PubMed PMID: 22444253; PubMed Central PMCID: PMC3328245.
4: Grisk O, Schlüter T, Reimer N, Zimmermann U, Katsari E, Plettenburg O, Löhn M, Wollert HG, Rettig R. The Rho kinase inhibitor SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. J Hypertens. 2012 May;30(5):980-9. doi: 10.1097/HJH.0b013e328351d459. PubMed PMID: 22388233.
5: Löhn M, Plettenburg O, Ivashchenko Y, Kannt A, Hofmeister A, Kadereit D, Schaefer M, Linz W, Kohlmann M, Herbert JM, Janiak P, O'Connor SE, Ruetten H. Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor. Hypertension. 2009 Sep;54(3):676-83. doi: 10.1161/HYPERTENSIONAHA.109.134353. Epub 2009 Jul 13. PubMed PMID: 19597037.
