JBSNF-000028,3026599-90-3

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JBSNF-000028 free base

CAS No. :

MCE 国际站：JBSNF-000028 free base

产品活性：JBSNF-000028 是一种具有口服活性的烟酰胺 N-甲基转移酶 (NNMT) 抑制剂，对人 NNMT (hNNMT)、猴 NNMT (mkNNMT) 和小鼠 NNMT (mNNMT) 的 IC₅₀ 分别为 0.033 μM、0.19 μM 和 0.21 μM。

研究领域：Others

作用靶点：Others

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

In Vivo: JBSNF-000028 (50 mg/kg; p.o.; twice daily for 27 days) improves glucose and lipid handling in mice with diet-induced obesity (DIO).
JBSNF-000028 (50 mg/kg; p.o.; twice daily for 4 weeks) improves glucose tolerance in NNMT knockout mice with diet-induced obesity.

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