For research use only. Not for therapeutic Use.
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].
DFBTA shows very weak cytotoxicity and cardiotoxicity (HEK293 proliferation IC50 > 30 μM, hERG IC50 > 30 μM)[1]
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].
| Catalog Number | I043619 |
| CAS Number | 2966044-07-3 |
| Synonyms | 4-(4-chlorophenyl)-2-[(2,5-difluorobenzoyl)amino]thiophene-3-carboxylic acid |
| Molecular Formula | C18H10ClF2NO3S |
| Purity | ≥95% |
| InChI | InChI=1S/C18H10ClF2NO3S/c19-10-3-1-9(2-4-10)13-8-26-17(15(13)18(24)25)22-16(23)12-7-11(20)5-6-14(12)21/h1-8H,(H,22,23)(H,24,25) |
| InChIKey | RZXHOVMOLRFUCA-UHFFFAOYSA-N |
| SMILES | C1=CC(=CC=C1C2=CSC(=C2C(=O)O)NC(=O)C3=C(C=CC(=C3)F)F)Cl |
| 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. |
