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Mofezolac

  Cat. No.:  DC12496   Featured
Chemical Structure
78967-07-4
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More than 5000 active chemicals with high quality for research!
Field of application
Mofezolac is a Highly Selective Cyclooxygenase-1 Inhibitors,Counteracting Inflammatory State both In Vitro and In Vivo Models of Neuroinflammation.
Cas No.: 78967-07-4
SMILES: COC1C=CC(C2C(C3C=CC(OC)=CC=3)=C(CC(O)=O)ON=2)=CC=1
Formula: C19H17NO5
M.Wt: 339.341985464096
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities[1].
Target: COX-1:1.44 nM (IC50) COX-2:447 nM (IC50)
In Vivo: Mofezolac (1-30 mg/kg; oral administration; once) treatment results in the suppression of writhing induced by the intraperitoneal injection of phenyl-p-benzoquinone in mice[1]. Animal Model: Female ddY mice (4 week old, 18-27 g) injected with phenyl-p-benzoquinone (PQ)[1] Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Oral administration; once Result: Dose-dependently suppressed the writhing induced by PQinjection in mice.
In Vitro: Mofezolac inhibits platelet aggregation with an IC50 of 0.45 μM in human platelet rich plasma (hPRP) assay[2]. Mofezolac slightly increase Bortezomib cytotoxic effect on multiple myeloma (MM) cell lines (NCI-H929 and RPMI-8226) and affects MM cell cycle and apoptosis when co-administered with the proteasome inhibitor Bortezomib[2].
References: [1]. K Goto, et al. Analgesic effect of mofezolac, a non-steroidal anti-inflammatory drug, against phenylquinone-induced acute pain in mice. Prostaglandins Other Lipid Mediat. 1998 Jul;56(4):245-54. [2]. Maria Laura Pati, et al. Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability. Eur J Med Chem. 2019 Feb 15;164:59-76.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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