A COX-1 selective NSAID (IC50s = 30 µM for COX-1

Tenidap – 5 mg

Brand:
Cayman
CAS:
120210-48-2
Storage:
-20
UN-No:
Non-Hazardous - /

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).{5386} It has anti-inflammatory and antirheumatic properties.{5386,34222} In vitro, it inhibits prostaglandin D2 (PGD2), leukotriene B4 (LTB4), and prostaglandin E2 (PGE2) synthesis (IC50s = 0.02, 18, and 32 µM, respectively).{34224,34225} Tenidap also reversibly and dose-dependently activates hKir2.3 channels in CHO cells (EC50 = 402 nM) and inhibits fatty acid amide hydrolase (FAAH) activity.{34223,25933} 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.  

 

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Description

A COX-1 selective NSAID (IC50s = 30 µM for COX-1, COX-2, and 5-LO, respectively); inhibits PGD2, LTB4, and PGE2 synthesis (IC50s = 0.02, 18, and 32 µM, respectively); activates hKir2.3 channels in CHO cells (EC50 = 402 nM); inhibits FAAH activity

Formal name: (3Z)-5-chloro-2,3-dihydro-3-(hydroxy-2-thienylmethylene)-2-oxo-1H-indole-1-carboxamide

Synonyms:  CP 66,248

Molecular weight: 320.8

CAS: 120210-48-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Cyclooxygenases||Product Type|Biochemicals|Small Molecule Inhibitors|Fatty Acid Metabolism||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Leukotrienes||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins

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