NCT-501 is a potent, reversible, theophylline-based inhibitor of ALDH1A1 (IC50 = 40 nM for the human form). It is selective for ALDH1A1 over other ALDH isozymes as well as other dehydrogenases. Pharmacokinetic studies indicate that NCT-501 has high bioavailability when delivered intraperitoneally, with rapid phase I modification in the liver.
yang s m, yasgar a, miller b, et al. discovery of nct-501, a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1a1 (aldh1a1)[j]. journal of medicinal chemistry, 2015, 58(15): 5967-5978.
