| Identification | Back Directory | [Name]
Acetamide, 2-[2-cyano-6-(1,1-dimethylethyl)phenoxy]-N-(4-hydroxyphenyl)- | [CAS]
2790481-63-7 | [Synonyms]
Nampt activator-3
2-(2-(tert-Butyl)-6-cyanophenoxy)-N-(4-hydroxyphenyl)acetamide
Acetamide, 2-[2-cyano-6-(1,1-dimethylethyl)phenoxy]-N-(4-hydroxyphenyl)- | [Molecular Formula]
C19H20N2O3 | [MOL File]
2790481-63-7.mol | [Molecular Weight]
324.37 |
| Chemical Properties | Back Directory | [Boiling point ]
596.1±50.0 °C(Predicted) | [density ]
1.22±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
9.96±0.26(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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 |
| Animal Model: | C57BL/6J mice[1] | | Dosage: | 1 or 3 mg/kg | | Administration: | IP; daily for one week followed by Taxol (18.3 mg/kg; ip; on day 9, 11, and 13) | | Result: | Showed a dose-dependent effect on elevation of paw withdrawal threshold.
Largely restored the density of myelinated fibers relative to the vehicle control group.
Significantly elevate NAD level in the sciatic nerves.
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| [References]
[1] Leibo Wang, et al. Optimization of NAMPT activators to achieve in vivo neuroprotective efficacy. Eur J Med Chem. 2022 Jun 5;236:114260. DOI:10.1016/j.ejmech.2022.114260 |
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