产品
编 号:F756019
分子式:C19H20N2O3
分子量:324.37
产品类型
结构图
CAS No: 2790481-63-7
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产品详情
生物活性:
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.
体内研究:
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。 Pharmacokinetic Parameters of NAMPT activator-3 in mice.IV (1 mg/kg)IP (30 mg/kg) PO (30 mg/kg)
Tmax (h)0.25
Cmax (ng/mL) 1563188
AUClast (h?ng/mL)1831333388
T1/2 (h)0.181.051.34
CL (mL/min/kg)90.4
Vss (mL/kg)1130
F (%)24.27.05
Animal Model:C57BL/6J mice
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.
体外研究:
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) 和肝癌细胞 (HepG2) 在内的细胞活力没有副作用。