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.