COX2-IN-1 |
カタログ番号GC32030
One-Click Copy Product Info
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Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 134729-13-8
Sample solution is provided at 25 µL, 10mM.
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COX2-IN-1 is a selective and inducible COX2 inhibitor with an IC50 of 0.24 μM. COX2-IN-1 is an anti-inflammatory compound with anti-inflammatory and analgesic activities.
COX2-IN-1 shows no COX-1 inhibition even at 100μM[1].
COX2-IN-1 has oral ED50 values of 0.030 and 0.47mg/kg on adjuvant-induced arthritis and collagen-induced arthritis, respectively, and an ED30 value of 7.4mg/kg in the yeast-induced hyperalgesia (Randall-Selitto) assay. COX2-IN-1 shows good analgesic activity and no ulcerogenicity[1].
[1]. Tsuji K, et al. Studies on anti-inflammatory agents. IV. Synthesis and pharmacological properties of 1,5-diarylpyrazoles and related derivatives. Chem Pharm Bull (1997), 45(6), 987-995.
Kinase experiment: | hCOX1 or hCOX2 is preincubated with COX2-IN-2 in 0.1 M Tris-HCl buffer containing 2 μM hematin and 5 mM L-tryptophan at 30°C for 5 min, followed by a 5 min incubation with arachidonic acid. The enzyme reaction is stopped by the addition of 1 N HCl. The PGE2 formed is extracted with EtOAc and measured by RIA[1]. |
Animal experiment: | Rats: Ten male Sprague Dawley rats are used per group. A suspension of 0.5% brewer's yeast in 0.5% methyl cellulose is injected into the right hind paw. The pain threshold us determined 3h after yeast injection. COX-2-IN-2 is given orally 2 h after yeast injection. The pain threshold in the treated rats are compared with that in the control rats[1]. |
References: [1]. Tsuji K, et al. Studies on anti-inflammatory agents. IV. Synthesis and pharmacological properties of 1,5-diarylpyrazoles and related derivatives. Chem Pharm Bull (1997), 45(6), 987-995. | |
| Cas No. | 134729-13-8 | SDF | |
| Canonical SMILES | N#CC1=NN(C2=CC=C(F)C=C2)C(C3=CC=C(S(=O)(C)=O)C=C3)=C1 | ||
| Formula | C17H12FN3O2S | M.Wt | 341.36 |
| 溶解度 | DMSO : 50 mg/mL (146.47 mM; Need ultrasonic) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9295 mL | 14.6473 mL | 29.2946 mL |
| 5 mM | 585.9 μL | 2.9295 mL | 5.8589 mL |
| 10 mM | 292.9 μL | 1.4647 mL | 2.9295 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 saline, 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)