Nampt-IN-5

Biological Activity

Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively[1]. Nampt-IN-5 (compound 27) (0-10 nM; 3 days) has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively [1].Nampt-IN-5 shows a good ADME data: mouse microsomal clearance (110 μl/min?mg), CYP3A4 inhibition value (0.75 μM), Sol6.8: 0.056 mM; MDCK Papp AB: 18.6[1]. Nampt-IN-5 (5-30 mg/kg; p.o. twice daily for 4 days) causes a significant amount of body weight loss in nude mice relative to vehicle[1].Nampt-IN-5 (10 mg/kg; p.o.) exhibits T1/2 (2.1 h), Cmax (29112 nM), and AUC (61984 nM?h) in mice[1].

References

[1]. Palacios DS, et al. Scaffold Morphing Identifies 3-Pyridyl Azetidine Ureas as Inhibitors of Nicotinamide Phosphoribosyltransferase (NAMPT).ACS Med Chem Lett. 2019 Oct 10;10(11):1524-1529.