Nampt activator-2

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].

Research Areas >> Neurological Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Nampt

Nampt activator-2 (compound 34) (10 μM, 4 h) 导致 A549 肺上皮细胞中 NMN 和 NAD 显着增加[1]。

Nampt activator-2 (compound 34) (1mg/kg 静脉注射和10mg /kg 口服，一次) 表现出低血浆清除率、良好的暴露和出色的口服生物利用度 (%F = 80)[1]。 Animal Model: Mouse[1] Dosage: 1 mg/kg iv and 10 mg/kg po Administration: IV, PO; once (Pharmacokinetic Analysis) Result: Pharmacokinetic Parameters of Nampt activator-2 in mouse[1]. IV (1 mg/kg) PO (10 mg/kg) Cmax (ng/mL) 9550 AUC0-24 (ng/mL∗h) 54463 t1/2 (h) 3.2 CL (mL/min/kg) 3 Vd (L/kg) 0.61 F (%) 80

[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.