化合物JBSNF-000028 T72947

Product Introduction
Bioactivity


英文名: JBSNF-000028

描述: JBSNF-000028 是一种具有口服活性和有效性的烟酰胺 N-甲基转移酶 (NNMT) 抑制剂，对人 NNMT (hNNMT)、猴 NNMT (mkNNMT) 和小鼠 NNMT (mNNMT) 具有抑制作用， IC50 分别为 0.033 μM、0.19 μM 和 0.21 μM。JBSNF-000028 可驱动胰岛素敏化、葡萄糖调节和体重减，可用于研究代谢紊乱。

体外活性: In U2OS cells, JBSNF-000028 hydrochloride (24 h) inhibits NNMT activity with an EC50 of 2.5 μM[1]. JBSNF-000028 hydrochloride (10-100 μM; 72 h) shows no cytotoxicity against HepG2 cells[1]. JBSNF-000028 hydrochloride binds below a hairpin structural motif at the nicotinamide pocket and stacks between Tyr-204 (from Hairpin) and Leu-164 (from the central domain)[1]. JBSNF-000028 hydrochloride is inactive against a broad panel of targets related to metabolism and safety[1].

体内活性: In mice with diet-induced obesity (DIO), JBSNF-000028 hydrochloride (50 mg/kg; oral; twice daily for 27 days) improves glucose and lipid handling[1]. JBSNF-000028 hydrochloride (50 mg/kg; oral; twice daily for 4 weeks) improves glucose tolerance in NNMT knockout mice with diet-induced obesity[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 3.85 mg/mL (20.54 mM)


相关库: Inhibitor Library

化合物JBSNF-000028 T72947信息由TargetMol中国为您提供，如您想了解更多关于化合物JBSNF-000028 T72947报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途