AMG 9810

AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat, respectively). Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine. In a rat model of inflammatory pain induced by intraplantar injection of complete Freund's adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia.Formal Name: (2E)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propenamide. CAS Number: 545395-94-6. Molecular Formula: C21H23NO3. Formula Weight: 337.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMSO: 16 mg/ml, Ethanol: 10 mg/ml. lambdamax: 304 nm. SMILES: CC(C)(C)C1=CC=C(/C=C/C(NC2=CC=C(OCCO3)C3=C2)=O)C=C1. InChi Code: InChI=1S/C21H23NO3/c1-21(2,3)16-7-4-15(5-8-16)6-11-20(23)22-17-9-10-18-19(14-17)25-13-12-24-18/h4-11,14H,12-13H2,1-3H3,(H,22,23)/b11-6+. InChi Key: GZTFUVZVLYUPRG-IZZDOVSWSA-N.