FR-188582 |
Catalog No.GC33893 |
FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC50 value of 17 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 189699-82-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | Human recombinant COX-1 and COX-2 are expressed in Chinese hamster ovary cells. The appropriate COX enzyme (1 μg for COX-1 and/or 3 μg for COX-2) is preincubated in 100 mM Tris-HCl buffer (pH 7.3) containing hematin (2 μM) and tryptophan (5 mM) with drugs (0.0001-100 μM) dissolved in 1% DMSO for 5 min at 37°C prior to the addition of Arachidonic acid (10 μM) for 5 min at 37°C. Reactions are terminated by the addition of 1N HCl, and PGE2 production is measured by radioimmunoassay[1]. |
Animal experiment: | Rats[1] Female Lewis rats (140-180g) at the age of 8 weeks are used. Adjuvant arthritis is induced in female Lewis rats by intradermal injection into the plantar suface of the right hind paw of 0.5 mg of a suspension of heat-killed and dried Mycobacterium tuberculosis H37 RA in 0.05 mL of liquid Paraffin (day 0). The drugs, suspended and diluted on 0.5% methylcellulose, are given orally once a day therapeutically from day 15 to day 24 after adjuvant injection. Paw volume is measured before and 15,18,21,24 days after adjuvant injection with the Volume Meter TK-105, and edema is expressed as the increase in paw volume after adjuvant injection relative to the pre-injection value for each animal.The anti-inflammatory effect is expressed as the difference in paw edema compared with that of vehicle-treated adjuvant-control rats. |
References: [1]. Ochi T, et al. The anti-inflammatory effect of FR188582, a highly selective inhibitor of cyclooxygenase-2, with an ulcerogenic sparing effect in rats. Jpn J Pharmacol. 2001 Feb;85(2):175-82. |
FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC50 value of 17 nM.
In a recombinant human cyclooxygenase (COX) enzyme activity, FR-188582 (FR188582) inhibits COX-2 with an IC50 value of 17 nM, and the inhibition of prostaglandin (PG) E2 formation by FR188582 isover 6000 times more selective for COX-2 than COX-1[1].
Oral administration of FR-188582 (0.01-3.2 mg/kg) reverses paw edema in adjuvant arthritic rats and shows a therapeutic effect in a dose-dependent manner with ED50 values (95% C.L.) of 0.074 (0.00021-0.53) and 0.063 (0.0039-0.31) mg/kg for adjuvant-injected paws and adjuvant-uninjected paws, respectively. The anti-inflammatory effect of FR-188582 (FR188582) is threefold more potent than that of Indomethacin with ED50 values (95% C.L.) of 0.24 (0.047-1.8) and 0.20 (0.021-0.79) mg/kg for adjuvant-injected paws and adjuvant-uninjected paws, respectively[1].
[1]. Ochi T, et al. The anti-inflammatory effect of FR188582, a highly selective inhibitor of cyclooxygenase-2, with an ulcerogenic sparing effect in rats. Jpn J Pharmacol. 2001 Feb;85(2):175-82.
Cas No. | 189699-82-9 | SDF | |
Canonical SMILES | O=S(C1=CC=C(C2=CC(Cl)=NN2C3=CC=CC=C3)C=C1)(C)=O | ||
Formula | C16H13ClN2O2S | M.Wt | 332.8 |
Solubility | Soluble in DMSO | 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 | 3.0048 mL | 15.024 mL | 30.0481 mL |
5 mM | 0.601 mL | 3.0048 mL | 6.0096 mL |
10 mM | 0.3005 mL | 1.5024 mL | 3.0048 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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 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.
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