1802088-50-1

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.

NCT-501 is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).

ALDH1

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.