| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S87621-100mg |
≥98% | ￥160.00 |
9 | - | - | - | - |
|
S87621-250mg |
≥98% | ￥259.00 |
货期：2-3天 | - | - | - | - |
|
S87621-1g |
≥98% | ￥660.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent and orally active Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s 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 | ||||||||||||||||||||
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| 靶点： | IC50: 1.8 µM (human NNMT), 2.8 µM (monkey NNMT) and 5.0 µM (mouse NNMT) | ||||||||||||||||||||
| 体外研究： | JBSNF-000088 (6-甲氧基烟酰胺) 对 U2OS 或分化的 3T3L1 细胞的 IC50 值为 1.6 μM 和 6.3 μM | ||||||||||||||||||||
| 体内研究： | JBSNF-000088 (6-甲氧基烟酰胺) (50 mg/kg；口服给药途径 4 周) 在第 21 天表现出具有统计学意义的体重 (%) 降低并导致进食血糖显著降低。 JBSNF-000088 (50 mg/kg；口服强饲法；每天两次，持续 4 周) 在第 28 天导致口服葡萄糖耐量显著改善，葡萄糖耐量正常化。 JBSNF-000088 (1 mg/kg；静脉内给药；持续 4 小时) 导致 21 mL/min·kg 的低血浆清除率和 0.7 L/kg 的稳态分布容积，非常短的血浆静脉内给药后的半衰期 (0.5 小时)。 JBSNF-000088 (10 mg/kg；口服灌胃；持续 4 小时) 导致 Cmax 为 3568 ng/mL，Tmax 值为 0.5 小时，表明在体内快速吸收肠道，口服灌胃的半衰期为 0.4 小时。发现口服生物利用度约为 40%。 Animal Model: Mice with high fat diet (HFD)-induced obesity Dosage: 50 mg/kg Administration: Oral route of administration for four weeks; oral gavage administration and twice daily for four weeks Result: Showed statistically significant reduction in body weight (%) and led to a statistically significant reduction in fed blood glucose on day 21 by oral route of administration.Led to a statistically significant improvement in oral glucose tolerance on day 28 with glucose tolerance being normalized by oral gavage administration. Animal Model: C57BL/6 mice Dosage: 1 mg/kg (Intravenous administration);10 mg/kg (oral gavage)(Pharmacokinetic Study) Administration: Intravenous administration and oral gavage; for 4 hours Result: Resulted 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 h upon intravenous administration.Resulted in a Cmax of 3568 ng/mL with a Tmax value of 0.5 hours, indicating rapid absorption in the intestine, and half-life of 0.4 hours by oral gavage. | ||||||||||||||||||||
| 参考文献： | 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. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO、H2O | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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