| Description | JBSNF-000028 TFA, a nicotinamide N-methyltransferase (NNMT) inhibitor, exhibits oral activity with inhibitory concentration 50 (IC50) values of 0.033 μM, 0.19 μM, and 0.21 μM for human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT) respectively. It is applicable in metabolic disorder research [1]. |
| In vitro | JBSNF-000028 TFA（24小时）在U2OS细胞中抑制NNMT活性，其EC50为2.5 μM [1]。在HepG2细胞中，JBSNF-000028 TFA（10-100μM；72小时）未显示出细胞毒性 [1]。JBSNF-000028 TFA能够结合在烟酰胺口袋的发夹结构基序下方，并在Tyr-204（来自发夹结构）与Leu-164（来自中心域）之间形成堆叠 [1]。对于与代谢和安全性相关的广泛靶点，JBSNF-000028 TFA均显示出无活性 [1]。 |
| In vivo | "JBSNF-000028 TFA（每日两次，口服，50 mg/kg，连续27天）能改善饮食诱导肥胖（DIO）小鼠的葡萄糖和脂质代谢[1]。同样的剂量和给药方式连续4周可以增强NNMT基因敲除导致的肥胖小鼠的葡萄糖耐受性[1]。" |
| molecular weight | 301.26 |
| Molecular formula | C13H14F3N3O2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |