| Bioactivity | JBSNF-000028 TFA is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 μM, 0.19 μM and 0.21 μM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 TFA can be used for the research of metabolic disorders[1]. |
| Target | IC50: 0.033 μM (hNNMT), 0.19 μM (mkNNMT), 0.21 μM (mNNMT) |
| Invitro | JBSNF-000028 TFA (24 h) inhibits NNMT activity with an EC50 of 2.5 μM in U2OS cells[1].JBSNF-000028 TFA (10-100 μM; 72 h) has no cytotoxicity against HepG2 cells[1].JBSNF-000028 TFA binds below a hairpin structural motif at the nicotinamide pocket and stacks between Tyr-204 (from Hairpin) and Leu-164 (from central domain)[1].JBSNF-000028 TFA is inactive against a broad panel of targets related to metabolism and safety[1]. |
| In Vivo | JBSNF-000028 TFA (50 mg/kg; p.o.; twice daily for 27 days) improves glucose and lipid handling in mice with diet-induced obesity (DIO)[1].JBSNF-000028 TFA (50 mg/kg; p.o.; twice daily for 4 weeks) improves glucose tolerance in NNMT knockout mice with diet-induced obesity[1]. |
| Name | JBSNF-000028 TFA |
| Formula | C13H14F3N3O2 |
| Molar Mass | 301.26 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ruf S, et al. Novel tricyclic small molecule inhibitors of Nicotinamide N-methyltransferase for the treatment of metabolic disorders. Sci Rep. 2022 Sep 14;12(1):15440. |