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    Bezafibrate
    Bezafibrate

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0836
    CAS #: 41859-67-0Purity ≥98%

    Description: Bezafibrate (BM 15075; BM-15075; Benzofibrate; BM15075; Bezalip; Bezatrol; Difaterol; Cedur; Bezafibratum) is an anti-hypertriglyceridemic/lipid-lowering drug acting. It acts as a potent agonist of PPAR (peroxisome proliferator-activated receptor alpha) with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ.  

    References: Mol Endocrinol. 1997 Jun;11(6):779-91; Diabetes. 2001 Aug;50(8):1883-90.

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    Molecular Weight (MW)361.82
    FormulaC19H20ClNO4
    CAS No.41859-67-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 72 mg/mL (199.0 mM)
    Water: <1 mg/mL
    Ethanol: 18 mg/mL (49.7 mM)
    Other info
    Chemical Name: 2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methyl-propanoic acid
    InChi Key: IIBYAHWJQTYFKB-UHFFFAOYSA-N
    InChi Code: InChI=1S/C19H20ClNO4/c1-19(2,18(23)24)25-16-9-3-13(4-10-16)11-12-21-17(22)14-5-7-15(20)8-6-14/h3-10H,11-12H2,1-2H3,(H,21,22)(H,23,24)
    SMILES Code: ClC1=CC=C(C(NCCC2=CC=C(OC(C)(C)C(O)=O)C=C2)=O)C=C1 
    SynonymsBM 15075; BM-15075; Bezafibrate; BM15075; Benzofibrate; Bezalip; Bezatrol; Difaterol; Cedur; Bezafibratum


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    In Vitro

    In vitro activity: Bezafibrate is a lipid-lowering fibric acid derivative. Bezafibrate binds to xPPARβ with EC50 of 5 μM. Bezafibrate transcriptionally activates the PPARβ of Xenopus with EC50 of 1 μM. Bezafibrate exposure to rat primary culture of adipocytes for 24 h increases the mRNA levels of crucial genes involved in peroxisomal and mitochondrial β-oxidation. The mRNA levels of the peroxisomal β-oxidation rate-limiting enzyme acyl-CoA oxidase and of the muscle-type carnitine palmitoyl transferase I (M-CPT-I) increases by 1.6-fold and 4.5-fold, respectively. Bezafibrate induces an increase in the transcript levels of the uncoupling protein-2 (UCP-2; 1.5-fold induction) and UCP-3 (3.7-fold induction), mitochondrial proteins that reduce ATP yield and may facilitate the oxidation of fatty acids. Furthermore, Bezafibrate increases the mRNA levels of the fatty acid translocase (2-fold induction). Bezafibrate causes a 1.9-fold induction in 9,10-[3H]palmitate oxidation. Moreover, Bezafibrate reduces the mRNA expression of several adipocyte markers, including PPARγ (30% reduction), tumor necrosis factor-α (33% reduction), and the ob gene (26% reduction). The reduction of the adipocyte markers causes by Bezafibrate is accompanied by an increase in the mRNA levels of the preadipocyte marker Pref-1 (1.6-fold induction).

    In VivoBezafibrate treatment is able to induce increasing mRNA levels of M-CPT-I (4.5-fold induction), fatty acid translocase (2.6-fold induction) and Pref-1 (5.6-fold induction) in epididymal white adipose tissue of rats. Similarly, increases. Bezafibrate feeding causes a significant increase in liver weight in wild-type and PPARβ-null mice compared to controls, while liver weight is unchanged in Bezafibrate-fed PPAR-α null mice. Gonadal adipose stores are significantly smaller in wild-type and PPARβ-null mice fed Bezafibrate than in controls (2.8-fold less and ~2.6-fold less, respectively), and this effect is not found in similarly fed PPARα-null mice. Bezafibrate is able to cause changes of mRNAs encoding lipid metabolizing enzymes (such as AOX , cytochrome P450 4A (CYP4A), LPL, ACS, and LCA D) in wild-type, PPARβ-null mice and PPARα-null mice compared to controls. Bezafibrate is able to induce UCPs expression, and modify energy homeostasis by directly inducing aco gene expression (14.5-fold at 7 days) and peroxisomal fatty acid β-oxidation in white adipose tissue of rats. Further, Bezafibrate significantly reduces plasma triglyceride and leptin concentrations, without modifying the levels of PPARγ or ob gene in white adipose tissue.
    Animal modelRats and mice
    Formulation & DosageTallyHo mice are bred in our animal facility. Only male mice are used in the study, and mice receive a standard diet (SD), which is supplemented with 0.5% (w/w) Bezafibrate for the Bezafibrate groups for 8 weeks. Animals are killed by isoflurane overdose, and dissected tissues are prepared as stated below. All data represent samples taken after 8 weeks of Bezafibrate (or SD) treatment unless otherwise stated
    ReferencesMol Endocrinol. 1997 Jun;11(6):779-91; Diabetes. 2001 Aug;50(8):1883-90; Franko A, et al. Bezafibrate ameliorates diabetes via reduced steatosis and improved hepatic insulin sensitivity in diabetic TallyHo mice. Mol Metab. 2017 Jan 6;6(3):256-266.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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