Elafibranor - CAS 923978-27-2
Catalog number: B0084-074234
Category: Inhibitor
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Elafibranor is a dual PPARα/δ agonist. Elafibranor increases plasma HDL and expression of Acox1, a PPARα target gene, and decreases plasma triglycerides and total cholesterol in the liver of ApoE2-KI wild-type mice. Elafibranor is identified as a drug candidate for the treatment of cardiometabolic diseases such as diabetes, insulin resistance, dyslipidemia, and non-alcoholic fatty liver disease (NAFLD).
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B0084-074234 250 mg $299 In stock
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PPARα/δ agonist
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Elafibranor; GFT505; GFT-505; GFT 505; 2-[2,6-dimethyl-4-[(E)-3-(4-methylsulfanylphenyl)-3-oxoprop-1-enyl]phenoxy]-2-methylpropanoic acid
potential treatment of cardiometabolic diseases
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1.Emerging drugs for hyperlipidemia.
Paras C;Hussain MM;Rosenson RS Expert Opin Emerg Drugs. 2010 Sep;15(3):433-51. doi: 10.1517/14728214.2010.481282.
IMPORTANCE OF THE FIELD: ;Elevated concentrations of low-density lipoprotein (LDL) cholesterol are associated with increased risk of coronary atherosclerosis, and morbidity and mortality from coronary heart disease (CHD). Lowering of LDL cholesterol leads to a reduction in cardiovascular morbidity and all-cause mortality in individuals at risk for cardiovascular events and patients with established CHD. The mainstays of lipid lowering therapy today are the HMG-CoA reductase inhibitors (statins); however, the residual risk of cardiovascular events amongst individuals treated with statins remains a major healthcare concern.;AREAS COVERED IN THIS REVIEW: ;Emerging targets for lipid lowering therapy target pathways that regulate lipoprotein assembly, lipoprotein clearance and pro-atherogenic lipoprotein modification. These emerging drugs have novel mechanisms that include inhibition of lipoprotein assembly (antisense mRNA inhibitors of apolipoprotein B and microsomal transfer protein inhibitors), enhanced lipoprotein clearance (proprotein convertase subtilisin kexin type 9, thyroid hormone analogues), inhibition of pro-atherogenic lipoprotein remodeling (cholesterol ester transfer protein inhibitors (dalcetrapib, anacetrapib) and peroxisome proliferator activator agents (GFT-505, aleglitazar)) and inhibition of lipoprotein modification (heme oxygenase-1 inhibitor (succinobucol), phospholipase A(2) inhibitors (varespladib, darapladib)).
2.Novel Pharmacotherapy Options for NASH.
Ratziu V Dig Dis Sci. 2016 May;61(5):1398-405. doi: 10.1007/s10620-016-4128-z. Epub 2016 Mar 22.
While simple to recommend, diet and lifestyle measures as a first-line therapy for nonalcoholic steatohepatitis (NASH) are hardly a model of successful therapy, as most clinicians can testify. They can be complex to implement, hard to sustain, and of limited efficacy in advanced stages of the disease. The need for specific pharmacotherapy is now acknowledged by practitioners, the pharmaceutical industry, and regulators and is largely expected by patients. The result is a clear move away from products developed second hand for NASH (such as pioglitazone or metformin) or from generic, non-specific hepatoprotectors (such as pentoxifylline, ursodeoxycholic acid, or antioxidants) toward molecules developed and tested specifically for NASH that aim to correct one or several of the pathways of liver injury in this disease. The two most advanced molecules, obeticholic acid and elafibranor, have shown encouraging data on improving hepatic histology. Both compounds appear to clear NASH, with obeticholic acid improving liver fibrosis and elafibranor improving the glycemic and lipid profile. Much larger trials, currently ongoing, will need to confirm these preliminary data and better characterize the safety and tolerability profile.
3.GFT505 for the treatment of nonalcoholic steatohepatitis and type 2 diabetes.
Cariou B;Staels B Expert Opin Investig Drugs. 2014 Oct;23(10):1441-8. doi: 10.1517/13543784.2014.954034. Epub 2014 Aug 28.
INTRODUCTION: ;PPARs are nuclear receptors that play key roles in the regulation of metabolism and inflammation. GFT505 is a new dual agonist of the PPARα and PPARδ isoforms, which improves lipid and glucose metabolism in type 2 diabetes mellitus (T2DM) and exerts hepatoprotective effects in mouse models of nonalcoholic fatty liver disease (NAFLD).;AREAS COVERED: ;This evaluation focuses on the pharmacology and clinical activity of GFT505 in metabolic diseases, including T2DM, dyslipidemia and NAFLD, as well as its promise as a therapeutic option for the treatment of nonalcoholic steatohepatitis. Original publications in English were selected, as well as abstracts of presentations in international congresses. Ongoing clinical trials were identified using the Clinicaltrial.gov database.;EXPERT OPINION: ;Results from the completed short-term (4 - 8 weeks) Phase IIa studies indicate that GFT505 decreases plasma triglyceride levels and increases high-density lipoprotein-cholesterol, while lowering low-density lipoprotein-cholesterol in prediabetic patients. Hyperinsulinemic-euglycemic clamp studies have also demonstrated an insulin-sensitizing effect of GFT505, with a strong effect on the liver, with a significant lowering effect on plasma liver enzymes.
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CAS 923978-27-2 Elafibranor

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