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JBSNF-000088

CAS No. : 7150-23-4

MCE 站：JBSNF-000088

产品活性：JBSNF-000088 (6-Methoxynicotinamide) 是烟酰胺 (NA) 的类似物，是一种有效的 NNMT (烟酰胺 N-甲基转移酶) 抑制剂，对人 NNMT，猴 NNMT 和小鼠 NNMT 的 IC₅₀ 分别为 1.8 ?M，2.8 ?M 和 5.0 ?M。在代谢性疾病的动物模型中，JBSNF-000088 抑制 NNMT 活性，降低 MNA 水平并驱动胰岛素增敏，调节葡萄糖和减轻体重。

研究领域：Metabolic Enzyme/Protease

作用靶点：Endogenous Metabolite

In Vitro: JBSNF-000088 (6-Methoxynicotinamide) has IC₅₀ values are 1.6 and 6.3??M for U2OS or differentiated 3T3L1 cells.

In Vivo: JBSNF-000088 (6-Methoxynicotinamide) (50?mg/kg; oral route of administration for four weeks) shows statistically significant reduction in body weight (%) and leads to a statistically significant reduction in fed blood glucose on day 21.
JBSNF-000088 (50?mg/kg; oral gavage administration; twice daily for four weeks) leads to a statistically significant improvement in oral glucose tolerance on day 28 with glucose tolerance being normalized.
JBSNF-000088 (1 mg/kg; intravenous administration; for 4 hours) results in low plasma clearance of 21?mL/min?kg and the volume of distribution at steady state of 0.7?L/kg, a very short plasma half-life of 0.5?hours upon intravenous administration.
JBSNF-000088 (10 mg/kg; oral gavage; for 4 hours) results in a Cmax of 3568 ng/mL with a T_max value of 0.5?hours, indicating rapid absorption in the intestine, and half-life of 0.4?hours by oral gavage. The oral bioavailability is found to be approximately 40%.

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