CAY10404 |
| カタログ番号GC43149 |
CAY10404 は、1 nM の IC50 と >500000 の選択指数 (SI; COX-1 IC50/COX-2 IC50) を持つ強力で選択的なシクロオキシゲナーゼ-2 (COX-2) 阻害剤です。
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Cas No.: 340267-36-9
Sample solution is provided at 25 µL, 10mM.
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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]
Reference:
[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(1), 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 Development Research 51, 273-286 (2000).
[3]. Mardini, I.A., and Fitzgerald, G.A. Selective inhibitors of cyclooxygenase-2: A growing class of anti-inflammatory drugs. Molecular Interventions 1(1), 30-38 (2001).
| Cas No. | 340267-36-9 | SDF | |
| Chemical Name | 3-[4-(methylsulfonyl)phenyl]-4-phenyl-5-(trifluoromethyl)-isoxazole | ||
| Canonical SMILES | FC(F)(F)c1onc(c2ccc(cc2)S(=O)(=O)C)c1c1ccccc1 | ||
| Formula | C17H12F3NO3S | M.Wt | 367.4 |
| 溶解度 | 17mg/mL in ethanol or DMSO, 21mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7218 mL | 13.6091 mL | 27.2183 mL |
| 5 mM | 0.5444 mL | 2.7218 mL | 5.4437 mL |
| 10 mM | 0.2722 mL | 1.3609 mL | 2.7218 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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