Nampt activator-3

• CAT Number: I041750
• CAS Number: 2790481-63-7
• Molecular Formula: C19H20N2O3
• Molecular Weight: 324.37
• Purity: ≥95%
• Synonyms: 2-(2-tert-butyl-6-cyanophenoxy)-N-(4-hydroxyphenyl)acetamide
• InChI: InChI=1S/C19H20N2O3/c1-19(2,3)16-6-4-5-13(11-20)18(16)24-12-17(23)21-14-7-9-15(22)10-8-14/h4-10,22H,12H2,1-3H3,(H,21,23)
• InChIKey: VKGWHNRIOPYZTC-UHFFFAOYSA-N
• SMILES: CC(C)(C)C1=CC=CC(=C1OCC(=O)NC2=CC=C(C=C2)O)C#N

NAMPT activator-3, a NAT derivative, is a NAMPT activator with an EC50 of 2.6 μM and a KD of 132 nM. NAMPT activator-3 effectively protects cultured cells from FK866 (HY-50876)-mediated toxicity. NAMPT activator-3 exhibits strong neuroprotective efficacy in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model without any overt toxicity[1].
NAMPT activator-3 (compound 72; 0.1, 0.3, 1, 3, 10 μM; 72 hours) exertes no side effect on the cell viability including osteosarcoma cells (U2OS), glioblastoma cells (T98G), neuroblastoma cells (SH-SY5Y) and liver carcinoma cells (HepG2)[1].
NAMPT activator-3 (compound 72) protects peripheral sensory neurons from Taxol (HY-B0015)-induced damage by enhancing NAD production[1].
Pharmacokinetic Parameters of NAMPT activator-3 in mice[1].

IV (1 mg/kg)
IP (30 mg/kg)
PO (30 mg/kg)

Tmax (h)

0.25

Cmax (ng/mL)

1563
188

AUClast (h∗ng/mL)
183
1333
388

T1/2 (h)
0.18
1.05
1.34

CL (mL/min/kg)
90.4

Vss (mL/kg)
1130

F (%)

24.2
7.05

Reference

[1]. Leibo Wang, et al. Optimization of NAMPT activators to achieve in vivo neuroprotective efficacy. Eur J Med Chem. 2022 Jun 5;236:114260.
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