中文名 | SAR407899 (hydrochloride) |
英文名 | SAR407899 (hydrochloride) |
别名 | 6-(4-哌啶基氧基)-1(2H)-异喹啉酮盐酸盐 6-(哌啶-4-氧基)异喹啉-1(2H)-酮盐酸盐 ROCK激酶抑制剂(SAR407899 HYDROCHLORIDE) |
英文别名 | SAR407899 SAR 407899 SAR-407899 SAR407899 HCl SAR407899 (hydrochloride) 6-(piperidin-4-yloxy)isoquinolin-1(2h)-one hcl 6-(4-Piperidinyloxy)-1(2H)-isoquinolinone hydrochloride 6-(piperidin-4-yloxy)isoquinolin-1(2H)-one hydrochloride |
CAS | 923262-96-8 |
化学式 | C14H17ClN2O2 |
分子量 | 280.74998 |
溶解度 | 溶于DMSO |
存储条件 | -20℃ |
产品用途 | 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. |
参考资料 展开查看 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.562 ml | 17.809 ml | 35.619 ml |
5 mM | 0.712 ml | 3.562 ml | 7.124 ml |
10 mM | 0.356 ml | 1.781 ml | 3.562 ml |
5 mM | 0.071 ml | 0.356 ml | 0.712 ml |
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