Acoramidis

Acoramidis is a kinetic stabilizer of transthyretin (TTR). It selectively binds to wild-type TTR and TTRV122I with negative cooperativity (Kd1s = 4.8 and 6.2 nM, respectively, Kd2s = 314 and 139 nM, respectively) over COX-1, COX-2, and the thyroid hormone nuclear receptor (IC50s = >10 µM for all). Acoramidis inhibits pH-induced amyloidogenesis of wild-type TTR and TTRV122I, indicating tetramer stabilization, when used at stoichiometric ratios of 1:1 and 1:0.5 with the number of TTR binding sites. It stabilizes TTRV122I in serum isolated from patients with familial amyloid cardiomyopathy when used at a concentration of 10 µM.Formal Name: 3-[3-(3,5-dimethyl-1H-pyrazol-4-yl)propoxy]-4-fluoro-benzoic acid. CAS Number: 1446711-81-4. Synonyms: AG-10. Molecular Formula: C15H17FN2O3. Formula Weight: 292.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Slightly soluble: 0.1-1 mg/ml. SMILES: O=C(C1=CC=C(C(OCCCC2=C(C)NN=C2C)=C1)F)O. InChi Code: InChI=1S/C15H17FN2O3/c1-9-12(10(2)18-17-9)4-3-7-21-14-8-11(15(19)20)5-6-13(14)16/h5-6,8H,3-4,7H2,1-2H3,(H,17,18)(H,19,20). InChi Key: WBFUHHBPNXWNCC-UHFFFAOYSA-N.