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CAY10404

Cayman Chemical Item Number 70210

CAY10404

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Description

Many non-steroidal anti-inflammatory drugs (NSAIDs) are potent but non-selective inhibitors of both COX-1 and COX-2 in humans.1 CAY10404 is one of the most selective inhibitors of COX-2 which has been reported to date, with a selectivity index (SI; SI = IC50 COX-1/IC50 COX-2) of >500,000. (The COX-1 IC50 is >500 mM, and COX-2 IC50 is <1 nM.)2 As a reference point, the SI of celecoxib is about 400. Thus, CAY10404 has an SI which is several logs greater than the first generation of selective COX-2 inhibitors, and is comparable to the SI of second generation selective COX-2 inhibitors, such as valdecoxib and etoricoxib.3

1 Barnett, J., Chow, J., Ives, D., et al. Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system. Biochim Biophys Acta 1209 130-139 (1994).

2 Habeeb, A.G., Rao, P.N.P., and Knaus, E.E. Design and syntheses of diarylisoxazoles: Novel inhibitors of cyclooxygenase-2 (COX-2) with analgesic-antiinflammatory activity. Drug Dev Res 51 273-286 (2000).

3 Mardini, I.A., and Fitzgerald, G.A. Selective inhibitors of cyclooxygenase-2: A growing class of anti-inflammatory drugs. Mol Interv 1 30-38 (2001).

Formal Name 3-​(4-​methylsulphonylphenyl)-​4-​phenyl-​5-​trifluoromethylisoxazole
Molecular Formula C17H12F3NO3S
Formula Weight 367.4
Formulation A crystalline solid
Purity >98%
λmax 239 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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FC(F)​(F)​c1onc(c2ccc(cc2)​S(=O)​(=O)​C)​c1c1ccccc1

Background Reading

Barnett, J., Chow, J., Ives, D., et al. Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system. Biochim Biophys Acta 1209 130-139 (1994).

Mardini, I.A., and Fitzgerald, G.A. Selective inhibitors of cyclooxygenase-2: A growing class of anti-inflammatory drugs. Mol Interv 1 30-38 (2001).

Habeeb, A.G., Rao, P.N.P., and Knaus, E.E. Design and syntheses of diarylisoxazoles: Novel inhibitors of cyclooxygenase-2 (COX-2) with analgesic-antiinflammatory activity. Drug Dev Res 51 273-286 (2000).
Size Price Quantity Subtotal
1 mg $18.00 $0.00
5 mg $81.00 $0.00
10 mg $144.00 $0.00
50 mg $630.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-05-26. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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