Celecoxib-d7 is intended for use as an internal standard for the quantification of celecoxib by GC- or LC-MS. Celecoxib is a selective inhibitor of COX-2 (IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively).1,2 It displays chemopreventive activity in multiple tumor types via proapoptotic effects that are independent of COX-2 inhibition.3,4,5 Formulations containing celecoxib have been used in the treatment of inflammation while circumventing the gastrointestinal toxicity associated with traditional non-sterodial anti-inflammatory drugs, however, the use of celecoxib has been tempered due to its ability to induce adverse cardiovascular events.6
1.Uddin, J.M., Rao, P.N.P., and Knaus, E.E.Design and synthesis of novel celecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: Replacement of the sulfonamide pharmacophore by a sulfonylazide bioisostereBioorg. Med. Chem.11(23)5273-5280(2003) 2.Mardini, I.A., and Fitzgerald, G.A.Selective inhibitors of cyclooxygenase-2: A growing class of anti-inflammatory drugsMolecular Interventions1(1)30-38(2001) 3.Jendrossek, V., Handrick, R., and Belka, C.Celecoxib activates a novel mitochondrial apoptosis signaling pathwayThe FASEB Journal171547-1549(2003) 4.Leahy, K.M., Ornberg, R.L., Wang, Y., et al.Cyclooxygenase-2 inhibition by celecoxib reduces proliferation and induces apoptosis in angiogenic endothelial cells in vivoCancer Research62625-631(2002) 5.Zhu, J., Huang, J.W., Tseng, P.H., et al.From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitorsCancer Res.644309-4318(2004) 6.Blobaum, A.L., and Marnett, L.J.Structural and functional basis of cyclooxygenase inhibitionJ. Med. Chem.50(7)1425-1441(2007)