| Bioactivity | DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain[1]. |
| Target | IC50: 0.024 ± 0.012 μM (ANO1), 8.7 ± 1.0 μM (ANO2) |
| Invitro | DFBTA shows very weak cytotoxicity and cardiotoxicity (HEK293 proliferation IC50 > 30 μM, hERG IC50 > 30 μM)[1] |
| In Vivo | DFBTA (C57BL/6 mice; 40-80 mg/kg, IG; 40 mg/kg, IV; once) shows weak acute toxicity, with mouse minimum lethal dosage (MLD) > 1000 mg/kg[1].DFBTA (C57BL/6 mice, 1000 mg/kg, Orally, once) shows excellent pharmacokinetics properties with oral bioavailability > 75% and little brain penetration (<1.5% brain/plasma)[1]. |
| Name | DFBTA |
| Formula | C18H10ClF2NO3S |
| Molar Mass | 393.79 |
| 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]. Wang Y, et al. Optimization of 4-arylthiophene-3-carboxylic acid derivatives as inhibitors of ANO1: Lead optimization studies toward their analgesic efficacy for inflammatory pain. Eur J Med Chem. 2022 Jul 5;237:114413. |