JBSNF-000088 (6-Methoxynicotinamide) 是烟酰胺 (NA) 的类似物，是一种口服有效的 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 µM，2.8 µM 和 5.0 µM。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。

JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent and orally active Nicotinamide N-methyltransferase (NNMT) inhibitor with IC 50 s of 1.8 μM, 2.8 μM, and 5.0?μM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease.

Solid

IC50: 1.8 μM (human NNMT), 2.8 μM (monkey NNMT) and 5.0?μM (mouse NNMT)

JBSNF-000088 (6-Methoxynicotinamide) has IC50 values are 1.6 and 6.3?μM for U2OS or differentiated 3T3L1 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

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-lif

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Kannt A, et al. A small molecule inhibitor of Nicotinamide N-methyltransferase for the treatment of metabolic disorders. Sci Rep. 2018 Feb 26;8(1):3660.

In Vitro: DMSO : ≥ 100 mg/mL (657.25 mM)H₂O : 1 mg/mL (6.57 mM; Need ultrasonic)