[CAS NO. 189699-82-9] FR-188582
PRODUCTS SPECIFICATIONS [189699-82-9]
DESCRIPTION [189699-82-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 332.80 |
| Molecular Formula | C16H13ClN2O2S |
| SMILES | O=S(C1=CC=C(C2=CC(Cl)=NN2C3=CC=CC=C3)C=C1)(C)=O |
Summary
FR-188582 is a highly selective inhibitor of cyclooxygenase ( COX )-2, with an IC 50 value of 17 nM.
IC50 & Target
|
COX-2 17 nM (IC 50 ) |
In Vitro
In a recombinant human cyclooxygenase (COX) enzyme activity, FR-188582 (FR188582) inhibits COX-2 with an IC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 ED 50 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 ED 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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 |