Nampt activator-2

• CAT Number: I041763
• CAS Number: 2237268-90-3
• Molecular Formula: C17H15ClN4O3S
• Molecular Weight: 390.84
• Purity: ≥95%
• Synonyms: 1-[4-(4-chlorophenyl)sulfonylphenyl]-3-(1H-pyrazol-4-ylmethyl)urea
• InChI: InChI=1S/C17H15ClN4O3S/c18-13-1-5-15(6-2-13)26(24,25)16-7-3-14(4-8-16)22-17(23)19-9-12-10-20-21-11-12/h1-8,10-11H,9H2,(H,20,21)(H2,19,22,23)
• InChIKey: WIQYSGZABYMFMD-UHFFFAOYSA-N
• SMILES: C1=CC(=CC=C1NC(=O)NCC2=CNN=C2)S(=O)(=O)C3=CC=C(C=C3)Cl

Nampt activator-2 (compound 34) is a potent NAMPT activator, with EC50 of 0.023 μM. Nampt activator-2 shows moderate activity against CYP2C9 (0.060 μM), 2D6 (0.41 μM) and 2C19 (0.59 μM)[1].
Nampt activator-2 (compound 34) (10 μM, 4 h) results in a marked increase of both NMN and NAD in A549 lung epithelial cells[1].
Nampt activator-2 (compound 34) (1 mg/kg iv and 10 mg/kg po, once) shows low plasma clearance, good exposure and excellent oral bioavailability (%F = 80)[1].

Reference

[1]. Pinkerton AB, et al. Optimization of a urea-containing series of nicotinamide phosphoribosyltransferase (NAMPT) activators. Bioorg Med Chem Lett. 2021 Jun 1;41:128007.
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