CAY10404 |
| Catalog No.GC43149 |
CAY10404는 IC50이 1nM이고 선택도 지수(SI; COX-1 IC50/COX-2 IC50)가 >500000인 강력하고 선택적인 시클로옥시게나제-2(COX-2) 억제제입니다.
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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 |
| Solubility | 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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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