1. Immunology/Inflammation
  2. COX
  3. FR-188582

FR-188582 

Cat. No.: HY-U00146 Purity: 99.21%
Handling Instructions

FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC50 value of 17 nM.

For research use only. We do not sell to patients.

FR-188582 Chemical Structure

FR-188582 Chemical Structure

CAS No. : 189699-82-9

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Description

FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC50 value of 17 nM.

IC50 & Target[1]

COX-2

17 nM (IC50)

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[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[1].

Molecular Weight

332.80

Formula

C₁₆H₁₃ClN₂O₂S

CAS No.

189699-82-9

SMILES

O=S(C1=CC=C(C2=CC(Cl)=NN2C3=CC=CC=C3)C=C1)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

FR-188582FR188582FR 188582COXCyclooxygenaseInhibitorinhibitorinhibit

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