AAT-008

AAT-008 is an orally bioavailable and potent antagonist of the prostaglandin E2 (PGE2) receptor subtype 4 (EP4, IC50 = 16.3 nM in a human EP4 functional assay). It is selective for EP4 with IC50 values of 2.4, 1,890, >20,000, and >20,000 nM for binding to human recombinant EP4, EP2, EP1, and EP3, respectively. AAT-008 has potent binding affinity for human, rat, and dog EP4 (Kis = 0.97, 6.1, and 38 nM, respectively) and suppresses PGE2-induced elevation of intracellular cAMP with an antagonistic potency (pA2) of 1.1 nM in vitro. Oral administration of AAT-008 reduces carrageenan-induced mechanical hyperalgesia in rats in a dose-dependent manner.Formal Name: 4-[(1S)-1-[[[5-chloro-2-(3-fluorophenoxy)-3-pyridinyl]carbonyl]amino]ethyl]-benzoic acid. CAS Number: 847727-81-5. Molecular Formula: C21H16ClFN2O4. Formula Weight: 414.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 234, 293 nm. SMILES: C[C@H](NC(C1=CC(Cl)=CN=C1OC2=CC=CC(F)=C2)=O)C3=CC=C(C(O)=O)C=C3. InChi Code: InChI=1S/C21H16ClFN2O4/c1-12(13-5-7-14(8-6-13)21(27)28)25-19(26)18-9-15(22)11-24-20(18)29-17-4-2-3-16(23)10-17/h2-12H,1H3,(H,25,26)(H,27,28)/t12-/m0/s1. InChi Key: FKXDPPYCCKCVCW-LBPRGKRZSA-N.