GS-9667 (CVT 3619), a novel N 6 -5'-substituted adenosine analog, is a selective, partial agonist of the A 1 adenosine receptor (A 1 AdoR) . GS-9667 binds to adipocyte membranes with high (K H =14 nM) and low (K L =5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC 50 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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