Nampt activator-3

Modify Date: 2024-01-12 17:56:12

Nampt activator-3 Structure
Nampt activator-3 structure
Common Name Nampt activator-3
CAS Number 2790481-63-7 Molecular Weight 324.37
Density N/A Boiling Point N/A
Molecular Formula C19H20N2O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Nampt activator-3


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].

 Names

Name Nampt activator-3

 Nampt activator-3 Biological Activity

Description 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].
Related Catalog
In Vitro NAMPT activator-3 (化合物 72; 0.1, 0.3, 1, 3, 10 μM; 72 小时) 对包括骨肉瘤细胞 (U2OS)、胶质母细胞瘤细胞 (T98G)、神经母细胞瘤细胞 (SH-SY5Y) 和肝癌在内的细胞活力没有副作用 细胞 (HepG2)[1]。
In Vivo NAMPT activator-3 (化合物 72; 1 or 3 mg/kg; 腹腔给药; 每天一次; 持续一周; 然后给药紫杉醇) 通过增强 NAD 的产生来保护外周感觉神经元免受紫杉醇 (HY-B0015) 诱导的损伤[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.
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.  

 Chemical & Physical Properties

Molecular Formula C19H20N2O3
Molecular Weight 324.37