A-939572 is a potent, specific and orally bioavailable SCD1 inhibitor with IC50 of <4 nM and 37 nM for rSCD1 and hSCD1, respectively.
A-939572 shows excellent selectivity and no significant hERG channel blockade activity (IC50>100 uM).
A-939572 prevents the diet-induced reduction of hepatic FAAH activity, normalizes hepatic AEA levels, and improves insulin sensitivity in HFD-fed mice.
A-939572 synergistically inhibits tumor growth in vitro and in vivo in combination with temsirolimus.
