Nampt-IN-5

• CAT Number: I016960
• CAS Number: 2380013-17-0
• Molecular Formula: C25H25N5O2
• Molecular Weight: 427.50
• Purity: ≥95%
• Synonyms: N-[4-[(2-ethoxybenzimidazol-1-yl)methyl]phenyl]-3-pyridin-3-ylazetidine-1-carboxamide
• InChI: InChI=1S/C25H25N5O2/c1-2-32-25-28-22-7-3-4-8-23(22)30(25)15-18-9-11-21(12-10-18)27-24(31)29-16-20(17-29)19-6-5-13-26-14-19/h3-14,20H,2,15-17H2,1H3,(H,27,31)
• InChIKey: JWEBCHOGBDMGBY-UHFFFAOYSA-N
• SMILES: CCOC1=NC2=CC=CC=C2N1CC3=CC=C(C=C3)NC(=O)N4CC(C4)C5=CN=CC=C5

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].

Reference

[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.
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