Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JBSNF-000028 是一种具有口服活性和有效性的烟酰胺 N-甲基转移酶 (NNMT) 抑制剂,对人 NNMT (hNNMT)、猴 NNMT (mkNNMT) 和小鼠 NNMT (mNNMT) 具有抑制作用, IC50 分别为 0.033 μM、0.19 μM 和 0.21 μM。JBSNF-000028 可驱动胰岛素敏化、葡萄糖调节和体重减,可用于研究代谢紊乱。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 2,350 | 现货 | ||
5 mg | ¥ 7,000 | 现货 | ||
10 mg | ¥ 8,550 | 现货 | ||
25 mg | ¥ 11,240 | 现货 | ||
50 mg | ¥ 13,800 | 现货 | ||
100 mg | ¥ 17,500 | 现货 |
产品描述 | JBSNF-000028 is an orally active and potent nicotinamide N-methyltransferase (NNMT) inhibitor with inhibitory effects on human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT) with IC50s of 0.033 μM, 0.19 μM, and 0.21 μM, respectively.JBSNF-000028 can drive insulin sensitization and weight loss. 000028 drives insulin sensitization, glucose regulation and weight loss and can be used to study metabolic disorders. |
靶点活性 | U2OS cells:2.5 μM (EC50) |
体外活性 | In U2OS cells, JBSNF-000028 hydrochloride (24 h) inhibits NNMT activity with an EC50 of 2.5 μM[1]. JBSNF-000028 hydrochloride (10-100 μM; 72 h) shows no cytotoxicity against HepG2 cells[1]. JBSNF-000028 hydrochloride binds below a hairpin structural motif at the nicotinamide pocket and stacks between Tyr-204 (from Hairpin) and Leu-164 (from the central domain)[1]. JBSNF-000028 hydrochloride is inactive against a broad panel of targets related to metabolism and safety[1]. |
体内活性 | In mice with diet-induced obesity (DIO), JBSNF-000028 hydrochloride (50 mg/kg; oral; twice daily for 27 days) improves glucose and lipid handling[1]. JBSNF-000028 hydrochloride (50 mg/kg; oral; twice daily for 4 weeks) improves glucose tolerance in NNMT knockout mice with diet-induced obesity[1]. |
别名 | JBSNF-000028 free base |
分子量 | 187.24 |
分子式 | C11H13N3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.85 mg/mL (20.54 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 5.3407 mL | 26.7037 mL | 53.4074 mL | 133.5185 mL |
5 mM | 1.0681 mL | 5.3407 mL | 10.6815 mL | 26.7037 mL | |
10 mM | 0.5341 mL | 2.6704 mL | 5.3407 mL | 13.3518 mL | |
20 mM | 0.267 mL | 1.3352 mL | 2.6704 mL | 6.6759 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
JBSNF-000028 Others JBSNF-000028 free base Inhibitor inhibitor inhibit