Gemfibrozil

SKU: orb1308681

Description

Gemfibrozil

Research Area

Metabolism Research, Molecular Biology, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 25812-30-0
• MW: 250.33
• Purity: 99.90%
• Formula: C₁₅H₂₂O₃
• SMILES: CC1=CC(OCCCC(C)(C)C(O)=O)=C(C)C=C1
• Target: Adrenergic Receptor,Cytochromes P450,PPAR
• Solubility: DMSO:250 mg/mL (998.68 mM);Ethanol:47 mg/mL (187.75 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.99 mM)

Bioactivity

• Target IC50:
  2C8:69 μM(Ki)|2C19:24 μM(Ki)|1A2:82 μM(Ki)|CYP2C9:5.8 μM(Ki)
• In Vivo:
  Gemfibrozil treatment significantly reduces (2-3-fold the plasma clearance of SVA an the biliary excretion of SVA glucuronide (together with its cyclization product SV), but no the excretion of a major oxidative metabolite of SVA in dogs.
• In Vitro:
  Gemfibrozil exerts a minimal inhibitory effect on CYP3A-mediated simvastatin hydroxy acid (SVA) oxidation, but does inhibit SVA glucuronidation in dog and human liver microsomes. Gemfibrozil markedly inhibits M-23 formation, with a K(i) (IC(50)) value of 69 (95) mM, whereas Inhibition of M-1 formation is weaker with a K(i) (IC(50)) value of 273 mM in human liver microsomes. Gemfibrozil strongly and competitively inhibits CYP2C9 activity, with a K(i) (IC(50)) value of 5.8 (9.6) mM. Gemfibrozil exhibits somewhat smaller inhibitory effects on CYP2C19 and CYP1A2 activities, with K(i) (IC(50)) Values of 24 (47) mM and 82 (136) mM, respectively Gemfibrozil, a lipid-lowering drug, inhibits cytokine-induced production of NO an the expression of inducible nitric-oxide synthase (iNOS) in human U373 mg astroglial cells and Primary astrocytes. Gemfibrozil induces peroxisome proliferator-responsive element (PPRE)-dependent luciferase activity, which is inhibited b the expression of DeltahPPAR-alpha the dominant-negative mutant of human PPAR-alpha. Gemfibrozil strongly inhibit the activation of NF-kappaB, AP-1, and C/EBPbeta but not that of gamma-activation site (GAS) in cytokine-stimulated astroglial cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Lopid, inhibit, Jezil, Gemfibrozil, Inhibitor, CI 719, CI719, CI-719, Decrelip, Cytochrome P450, CYPs, CYP1A2, CYP2C9, AdrenergicReceptor, Adrenergic Receptor, Peroxisome proliferator-activated receptors, PPAR, PPARα

Compound Identifiers

PubChem CID

3463