FR122047 (hydrochloride)

FR122047 is a selective inhibitor of COX-1. The IC50 values for inhibition of human COX-1 and COX-2 are 0.028 and 65 µM, respectively. In human platelet-rich plasma, FR122047 inhibits arachidonic acid, collagen, and ADP-induced platelet aggregation with an IC50 of 180-200 nM, which is nearly 100 times more potent than aspirin. Unlike aspirin, FR122047 does not induce gastric damage upon oral administration at doses (100 mg/kg) far in excess of the dose needed for complete suppression of platelet COX-1. In some models of inflammation, such as collagen-induced arthritis in the rat, FR122047 has an anti-inflammatory effect, implying a role for COX-1 in these models.Formal Name: 1-[[4,5-bis(4-methoxyphenyl)-2-thiazolyl]carbonyl]-4-methyl-piperazine, monohydrochloride. CAS Number: 130717-51-0. Molecular Formula: C23H25N3O3S . HCl. Formula Weight: 460.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMF:PBS (pH 7.2) (1:10): 100 µg/ml, DMSO: 1 mg/ml. lambdamax: 234, 270, 344 nm. SMILES: O=C(N1CCN(C)CC1)C2=NC(C3=CC=C(OC)C=C3)=C(S2)C4=CC=C(OC)C=C4.Cl. InChi Code: InChI=1S/C23H25N3O3S.ClH/c1-25-12-14-26(15-13-25)23(27)22-24-20(16-4-8-18(28-2)9-5-16)21(30-22)17-6-10-19(29-3)11-7-17,/h4-11H,12-15H2,1-3H3,1H. InChi Key: YWMAVHIKOAOSFM-UHFFFAOYSA-N.