Bezafibrate

Catalog No.S4159 Batch:S415901

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Technical Data

Formula

C19H20ClNO4
Molecular Weight 361.82 CAS No. 41859-67-0
Solubility (25°C)* In vitro DMSO 72 mg/mL (198.99 mM)
Ethanol 18 mg/mL (49.74 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Bezafibrate (BM 15075) is the first clinically tested dual and pan-PPAR co-agonism.
Targets
PPAR [1]
In vitro 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. [1] 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). [2]
In vivo Bezafibrate 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. [2] 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. [3] 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. [4]

Protocol (from reference)

Selleck's Bezafibrate has been cited by 2 publications

Defective metabolic programming impairs early neuronal morphogenesis in neural cultures and an organoid model of Leigh syndrome [ Nat Commun, 2021, 12(1):1929] PubMed: 33771987
Targeting the EZH2-PPAR Axis Is a Potential Therapeutic Pathway for Pancreatic Cancer [ PPAR Res, 2021, 2021:5589342] PubMed: 34335707

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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