MedChemExpress LLC (MCE)

MedChemExpressModel Pelubiprofen - 69956-77-0

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Pelubiprofen is an orally active anti-inflammatory agent that inhibits COX enzyme activity (with IC50 values of 10.66 and 2.88 μM for COX-1 and COX-2, respectively). Pelubiprofen has significant anti-inflammatory and analgesic effects[1][2].
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Pelubiprofen

MCE China:Pelubiprofen

Brand:MedChemExpress (MCE)

Cat. No.HY-12383

CAS:69956-77-0

Purity:99.27%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Pelubiprofen is an orally active anti-inflammatory agent that inhibits COX enzyme activity (with IC50 values of 10.66 and 2.88 μM for COX-1 and COX-2, respectively). Pelubiprofen has significant anti-inflammatory and analgesic effects.

In Vitro:Pelubiprofen (0.01-60 μM, 24 h) inhibits COX in RAW 264.7 cells and suppresses LPS (HY-D1056)-induced PGE2 (IC50 is 0.13 μM)[1]. Pelubiprofen (15-60 μM, 24 h) inhibits the expression of iNOS and pro-inflammatory cytokines induced by LPS (HY-D1056) in RAW 264.7 cells[1]. Pelubiprofen (15-60 μM, 24 h) suppresses the activation of NF-κB induced by LPS (HY-D1056) in RAW 264.7 cells[1]. Pelubiprofen (15-60 μM, 24 h) inhibits IKK and TAK1 in RAW 264.7 cells induced by LPS (HY-D1056)[1].

In Vivo:Pelubiprofen (25-100 mg/kg, oral, single dose) inhibits the anti-inflammatory effect of NF-κB in the carrageenan-induced paw edema model[1].

IC50 & Target:COX-2 TAK1

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References:

[1]. Ji-Sun Shin, et al. Anti-inflammatory effect of pelubiprofen, 2-[4-(oxocyclohexylidenemethyl)-phenyl]propionic acid, mediated by dual suppression of COX activity and LPS-induced inflammatory gene expression via NF-κB inactivation. J Cell Biochem. 2011 Dec;112(12):3594-603.  [Content Brief]

[2]. Choi IA, Baek HJ, et al. Comparison of the efficacy and safety profiles of a pelubiprofen versus celecoxib in patients with rheumatoid arthritis: a 6-week, multicenter, randomized, double-blind, phase III, non-inferiority clinical trial. BMC Musculoskelet Disord. 2014 Nov 18;15:375.  [Content Brief]

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