GS-9667 Chemical Properties

Boiling point:

752.4±70.0 °C(Predicted)

Density 

1.68±0.1 g/cm3(Predicted)

pka

13.09±0.70(Predicted)

form 

Solid

color 

Light yellow to yellow

GS-9667 Usage And Synthesis

Uses

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].

References

[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. DOI:10.1124/jpet.105.099119
[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. DOI:10.1002/jcph.9