| Bioactivity | 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]. |
| CAS | 618380-90-8 |
| Formula | C21H24FN5O4S |
| Molar Mass | 461.51 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. |