FR-188582
FR-188582 Basic information
- Product Name:
- FR-188582
- Synonyms:
-
- FR-188582
- 1H-Pyrazole, 3-chloro-5-[4-(methylsulfonyl)phenyl]-1-phenyl-
- FR 188582,FR188582
- CAS:
- 189699-82-9
- MF:
- C16H13ClN2O2S
- MW:
- 332.8
- Mol File:
- 189699-82-9.mol
FR-188582 Chemical Properties
- Boiling point:
- 539.7±50.0 °C(Predicted)
- Density
- 1.33±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- pka
- -3.80±0.10(Predicted)
- color
- Light yellow to yellow
FR-188582 Usage And Synthesis
Uses
FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC50 value of 17 nM.
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].
IC 50
COX-2: 17 nM (IC50)
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. DOI:10.1254/jjp.85.175
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