618380-90-8
Chemical Structure
GS-9667
Synonym(s): CVT 3619
- CAS No.: 618380-90-8
- Formula:C21H24FN5O4S
- Molecular Weight:461.51
IUPAC Name: (2S,3S,4R,5R)-2-(((2-fluorophenyl)thio)methyl)-5-(6-(((1R,2R)-2-hydroxycyclopentyl)amino)-9H-purin-9-yl)tetrahydrofuran-3,4-diol
InChIKey: IZRXENCTXNMAMI-DIJFLQFKSA-N
SMILES: O[C@H]1[C@@H](O[C@@H]([C@H]1O)CSC2=C(C=CC=C2)F)N3C4=NC=NC(N[C@H]5[C@@H](CCC5)O)=C4N=C3
Biological Activity: GS-9667 (CVT 3619), a novel N6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA)[1][2].
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GS-9667 | 98.08% | GS-9667 (CVT 3619), a novel N6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA). | ||||||||||||||||||||
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- [1]. Marjan Fatholahi, et al. A novel partial agonist of the A(1)-adenosine receptor and evidence of receptor homogeneity in adipocytes. J Pharmacol Exp Ther. 2006 May;317(2):676-84. [Content Brief]
- [2]. Peter M Staehr, et al. Reduction of free fatty acids, safety, and pharmacokinetics of oral GS-9667, an A(1) adenosine receptor partial agonist. J Clin Pharmacol. 2013 Apr;53(4):385-92. [Content Brief]
Keywords
