Tenidap

Tenidap is a COX-1 selective non-steroidal anti-inflammatory drug (IC50s = 30 µM for COX-1, COX-2, and 5-lipoxygenase (5-LO), respectively). It has anti-inflammatory and antirheumatic properties. In vitro, it inhibits prostaglandin D2 (PGD2), leukotriene B4 (LTB4), and prostaglandin E2 (PGE2) synthesis (IC50s = 0.02, 18, and 32 µM, respectively). Tenidap also reversibly and dose-dependently activates hKir2.3 channels in CHO cells (EC50 = 402 nM) and inhibits fatty acid amide hydrolase (FAAH) activity. A formulation containing tenidap was not approved for rheumatoid and osteoarthritis by the FDA due to adverse effects, including bone mineralization loss, as well as liver and kidney toxicity.Formal Name: (3Z)-5-chloro-2,3-dihydro-3-(hydroxy-2-thienylmethylene)-2-oxo-1H-indole-1-carboxamide. CAS Number: 120210-48-2. Synonyms: CP 66,248. Molecular Formula: C14H9ClN2O3S. Formula Weight: 320.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 20 mg/ml, Ethanol: slightly soluble. lambdamax: 219, 273, 370 nm. SMILES: NC(N(C1=CC=C(Cl)C=C1/C2=C(C3=CC=CS3)/O)C2=O)=O. InChi Code: InChI=1S/C14H9ClN2O3S/c15-7-3-4-9-8(6-7)11(13(19)17(9)14(16)20)12(18)10-2-1-5-21-10/h1-6,18H,(H2,16,20)/b12-11-. InChi Key: LXIKEPCNDFVJKC-QXMHVHEDSA-N.