An inhibitor of COX-2 and carbonic anhydrase; inhibits COX-2 (IC50 = 40 nM in the absence of CAII) with lower inhibition in the presence of a CAII; prevents prostaglandin E2 (PGE2) production by >95 and 90% in HCA-7 and HT-29 human colon cancer cells

Polmacoxib – 5 mg

Brand:
Cayman
CAS:
301692-76-2
Storage:
-20
UN-No:
Non-Hazardous - /

Polmacoxib is an inhibitor of cyclooxygenase 2 (COX-2) and the carbonic anhydrase subtypes I (CAI) and CAII.{38663} It inhibits COX-2 in the absence of carbonic anhydrase II with an IC50 value of 40 nM, which increases by approximately 4- and 17-fold in the presence of a CAII at a molar ratio of 1:1 and 1:5, respectively.{38665} It also inhibits CAI and CAII (IC50s = 210 and 95 nM, respectively). Polmacoxib prevents >95 and 90% of prostaglandin E2 (PGE2) production in HCA-7 and HT-29 human colon cancer cells, respectively, using concentrations of 0.01 and 0.001 µg/ml.{38664} It inhibits polyp formation in a transgenic mouse model of intestinal polyp formation and tumor growth in human colorectal carcinoma mouse xenograft models when used at a dose of 7 mg/kg. The inhibition of COX-2 and CAII by polmacoxib has the potential for fewer serious systemic adverse effects, including cardiovascular events associated with COX-2 selective inhibitors such as celecoxib (Item No. 10008672).{38663,38665} Formulations containing polmacoxib have been used in the treatment of osteoarthritis.  

 

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Description

An inhibitor of COX-2 and carbonic anhydrase; inhibits COX-2 (IC50 = 40 nM in the absence of CAII) with lower inhibition in the presence of a CAII; prevents prostaglandin E2 (PGE2) production by >95 and 90% in HCA-7 and HT-29 human colon cancer cells, respectively (0.01 and 0.001 µg/ml); inhibits polyp formation and tumor growth (7 mg/kg)

Formal name: 4-[3-(3-fluorophenyl)-4,5-dihydro-5,5-dimethyl-4-oxo-2-furanyl]-benzenesulfonamide

Synonyms: 

Molecular weight: 361.4

CAS: 301692-76-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Carbonic Anhydrase||Product Type|Biochemicals|Small Molecule Inhibitors|Cyclooxygenases||Research Area|Cancer||Research Area|Immunology & Inflammation|Arthritis (Non-autoimmune)||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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