An agonist of PPARα and PPARδ; increases HDL secretion and expression of lipid-related genes ABCA1

Elafibranor – 10 mg

Brand:
Cayman
CAS:
923978-27-2
Storage:
-20
UN-No:
Non-Hazardous - /

Elafibranor is an agonist of the peroxisome proliferator-activated receptors (PPAR) α and δ.{37274} It increases HDL secretion and expression of the lipid-related genes ABCA1, PLIN2, and ABHD5 in Caco-2/TC7 cells in a PPARα-dependent manner. Elafibranor (10 mg/kg) decreases levels of plasma triglycerides and total cholesterol while increasing plasma HDL and expression of Acox1, a PPARα target gene, in the liver of ApoE2-KI wild-type, but not PPARα knockout, mice fed a Western diet. However, PPARα knockout mice exhibit a decrease in plasma total and non-HDL cholesterol levels, indicating PPARδ has a role in these functions. Elafibranor (30 mg/kg) reduces diet-induced macro- and micro-steatosis in a PPARα-deficient mouse model of non-alcoholic steatohepatitis.{37275} It also reduces cholesterol and triglyceride accumulation as well as macrovesicular steatosis in the liver of insulin-resistant db/db mice fed the methionine-choline deficient (MCD) diet. Formulations containing elafibranor are under clinical investigation for the treatment of non-alcoholic steatohepatitis.  

 

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Description

An agonist of PPARα and PPARδ; increases HDL secretion and expression of lipid-related genes ABCA1, PLIN-2, and ABHD5 in Caco-2/TC7 cells in a PPARα-dependent manner; decreases levels of plasma triglycerides and total cholesterol while increasing plasma HDL and expression of Acox1 in the liver of ApoE2-KI wild-type, but not PPARα knockout, mice fed a Western diet when administered at a dose of 10 mg/kg; reduces diet-induced macro- and micro-steatosis in a PPARα-deficient mouse model of non-alcoholic steatohepatitis; reduces cholesterol and triglyceride accumulation as well as macrovesicular steatosis in the liver of insulin-resistant db/db mice fed the MCD diet

Formal name: 2-[2,6-dimethyl-4-[(1E)-3-[4-(methylthio)phenyl]-3-oxo-1-propen-1-yl]phenoxy]-2-methyl-propanoic acid

Synonyms:  GFT505

Molecular weight: 384.5

CAS: 923978-27-2

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|PPARs||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Dyslipidemias||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity

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