Description
FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC50 value of 17 nM.
Product information
CAS Number: 189699-82-9
Molecular Weight: 332.80
Formula: C16H13ClN2O2S
Chemical Name: 3-chloro-5-(4-methanesulfonylphenyl)-1-phenyl-1H-pyrazole
Smiles: CS(=O)(=O)C1C=CC(=CC=1)C1=CC(Cl)=NN1C1C=CC=CC=1
InChiKey: YKHNOHGHDAQJFW-UHFFFAOYSA-N
InChi: InChI=1S/C16H13ClN2O2S/c1-22(20,21)14-9-7-12(8-10-14)15-11-16(17)18-19(15)13-5-3-2-4-6-13/h2-11H,1H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
In Vivo:
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.
Products are for research use only. Not for human use.
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