Description
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.
Product information
CAS Number: 2380013-17-0
Molecular Weight: 427.50
Formula: C25H25N5O2
Chemical Name: N-{4-[(2-ethoxy-1H-1,3-benzodiazol-1-yl)methyl]phenyl}-3-(pyridin-3-yl)azetidine-1-carboxamide
Smiles: CCOC1=NC2=CC=CC=C2N1CC1C=CC(=CC=1)NC(=O)N1CC(C1)C1=CN=CC=C1
InChiKey: JWEBCHOGBDMGBY-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (116.96 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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 . 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.
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. Nampt-IN-5 (10 mg/kg; p.o.) exhibits T1/2 (2.1 h), Cmax (29112 nM), and AUC (61984 nM•h) in mice.
Products are for research use only. Not for human use.
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