产品
编 号：F435064
分子式：C7H8N2O2
分子量：152.15
分子式：C7H8N2O2
分子量：152.15
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
100mg
询价
询价
结构图
CAS No: 7150-23-4
产品详情
生物活性：
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.
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.
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。
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.
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.
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。
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