SC-560

SC-560 is a member of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors which includes celecoxib (Celebrex(TM)) and rofecoxib (Vioxx(TM)). However, unlike these selective COX-2 inhibitors, SC-560 is a selective inhibitor of COX-1. Using human recombinant enzymes, the IC50 value for SC-560 with respect to COX-1 is 9 nM, while the corresponding IC50 value for COX-2 is 6.3 µM. Thus, SC-560 shows 700-fold selectivity for the COX-1 enzyme. SC-560 is orally active in the rat, where 10 mg/kg completely abolishes the ionophore-induced production of thromboxane B2 in whole blood. However, SC-560 is ineffective in the treatment of inflammation in models such as the LPS-induced rat air-pouch model, in which the COX-2 generated prostaglandins play a significant role in the inflammatory process. In whole cells, however, SC-560 appears to act as a non-selective COX inhibitor. The mechanism of the selective versus non-selective effects of SC-560 in a cell-free environment compared whole cells has not been elucidated.Formal Name: 5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole. CAS Number: 188817-13-2. Molecular Formula: C17H12ClF3N2O. Formula Weight: 352.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 150 mg/ml, DMF:PBS (1:1): 1.2 mg/ml, DMSO: 24 mg/ml, Ethanol: 22 mg/ml. lambdamax: 232, 251 nm. SMILES: COc1ccc(cc1)n1nc(cc1c1ccc(Cl)cc1)C(F)(F)F. InChi Code: InChI=1S/C17H12ClF3N2O/c1-24-14-8-6-13(7-9-14)23-15(10-16(22-23)17(19,20)21)11-2-4-12(18)5-3-11/h2-10H,1H3. InChi Key: PQUGCKBLVKJMNT-UHFFFAOYSA-N.