| Chemical Properties | Back Directory | [density ]
1.29±0.1 g/cm3(Predicted) | [solubility ]
DMSO : 50 mg/mL (116.96 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.75±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | [in vivo]
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]. | [IC 50]
CYP3: 0.7 nM (IC50) | [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. |
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