Sulindac-d3 (Synonyms: MK-231-d3)

Sulindac-d₃ is intended for use as an internal standard for the quantification of sulindac by GC- or LC-MS. Sulindac is a non-steroidal anti-inflammatory drug (NSAID), selective COX-2 inhibitor (IC₅₀s = 0.79 and >1,000 µM for COX-2 and COX-1, respectively), and prodrug form of sulindac sulfide .^1,2,3,4 Sulindac is reduced by intestinal bacteria to form sulindac sulfide.¹ It inhibits acetic acid-induced writhing in mice and reduces paw edema induced by carrageenan in rats when administered at a dose of 100 mg/kg.³ Sulindac (60 mg/kg) reduces tumor growth in MiaPaCa-2 and BxPC-3 mouse xenograft models.⁴ Formulations containing sulindac have been used in the treatment of pain associated with arthritis, ankylosing spondylitis, and gout.

1.Maseda, D., and Ricciotti, E.NSAID-gut microbiota interactionsFront. Pharmacol.111153(2020) 2.Grossman, C.J., Wiseman, J., Lucas, F.S., et al.Inhibition of constitutive and inducible cyclooxygenase activity in human platelets and mononuclear cells by NSAIDs and Cox 2 inhibitorsInflamm. Res.44(6)253-257(1995) 3.Bhat, M.A., Al-Omar, M.A., Alsaif, N.A., et al.Novel sulindac derivatives: Synthesis, characterisation, evaluation of antioxidant, analgesic, anti-inflammatory, ulcerogenic and COX-2 inhibition activityJ. Enzyme Inhib. Med. Chem.35(1)921-934(2020) 4.Yip-Schneider, M.T., Wu, H., Ralstin, M., et al.Suppression of pancreatic tumor growth by combination chemotherapy with sulindac and LC-1 is associated with cyclin D1 inhibition in vivoMol. Cancer Ther.6(6)1736-1744(2007)