Pemafibrate - CAS 848259-27-8
Catalog number: B0084-476656
Category: Inhibitor
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Pemafibrate is a Peroxisome proliferator-activated receptor alpha agonist. It can decrease the secretion of inflammatory markers without affecting cell proliferation or tube formation. Pemafibrate was associated with the inhibition of inflammatory responses without affecting cell proliferation or angiogenesis, and subsequently may induce an anti-atherosclerotic effect. In Jan 2017, Phase-III clinical trials in Dyslipidaemias in USA were on-going.
(R)K-13675;(R)-2-(3-((benzo[d]oxazol-2-yl(3-(4-methoxyphenoxy)propyl)amino)methyl)phenoxy)butanoic acid
Soluble in DMSO
-20℃ Freezer
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
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Current Developer:
Originator Kowa Pharmaceutical
1.Current and future pharmacological therapies for NAFLD/NASH.
Sumida Y;Yoneda M J Gastroenterol. 2018 Mar;53(3):362-376. doi: 10.1007/s00535-017-1415-1. Epub 2017 Dec 16.
Nonalcoholic fatty liver disease (NAFLD) is the most prevalent liver disease worldwide, and there is no approved pharmacotherapy. The efficacy of vitamin E and pioglitazone has been established in nonalcoholic steatohepatitis (NASH), a progressive form of NAFLD. GLP-1RA and SGLT2 inhibitors, which are currently approved for use in diabetes, have shown early efficacy in NASH, and also have beneficial cardiovascular or renal effects. Innovative NASH therapies include four main pathways. The first approach is targeting hepatic fat accumulation. Medications in this approach include modulation of peroxisome proliferator-activator receptors (e.g., pemafibrate, elafibranor), medications targeting farnesoid X receptor axis [obeticholic acid; OCA)], inhibitors of de novo lipogenesis (aramchol, ACC inhibitor), and fibroblast growth factor-21 analogues. A second target is oxidative stress, inflammation, and apoptosis. This class of drug includes apoptosis signaling kinase 1 (ASK1) inhibitor and emricasan (an irreversible caspase inhibitor). A third target is intestinal microbiomes and metabolic endotoxemia. Several agents are in ongoing trials, including IMMe124, TLR4 antagonist, and solithromycin (macrolide antibiotics).
2.New oral agents for treating dyslipidemia.
Gryn SE;Hegele RA Curr Opin Lipidol. 2016 Dec;27(6):579-584.
PURPOSE OF REVIEW: ;We provide an overview of orally administered lipid-lowering therapies under development.;RECENT FINDINGS: ;Recent data support statins for intermediate risk primary prevention, and ezetimibe for high-risk secondary prevention. Novel agents in development include bempedoic acid and gemcabene, and work continues on one remaining cholesteryl ester transfer protein inhibitor, anacetrapib, to determine whether this class can reduce cardiovascular risk. Selective peroxisome proliferator-activated receptor modulators such as K-877 are under study to determine whether they have an advantage over older fibrates. Diacylglycerol transferase inhibitors such as pradigastat appear to have potent triglyceride-lowering effects, even for patients with familial chylomicronemia syndrome. Finally, novel ω-3 preparations are available with significant triglyceride lowering, although their role in therapy remains unclear.;SUMMARY: ;Statins will remain the backbone of lipid-lowering therapy, although several novel oral agents are promising. The common theme across drugs in development is the demonstration of good lipid-lowering effect, although lacking cardiovascular outcomes data, which will likely be necessary before any of them, can be recommended or approved for widespread use.
3.PPAR Agonists and Metabolic Syndrome: An Established Role?
Botta M;Audano M;Sahebkar A;Sirtori CR;Mitro N;Ruscica M Int J Mol Sci. 2018 Apr 14;19(4). pii: E1197. doi: 10.3390/ijms19041197.
Therapeutic approaches to metabolic syndrome (MetS) are numerous and may target lipoproteins, blood pressure or anthropometric indices. Peroxisome proliferator-activated receptors (PPARs) are involved in the metabolic regulation of lipid and lipoprotein levels, i.e., triglycerides (TGs), blood glucose, and abdominal adiposity. PPARs may be classified into the α, β/δ and γ subtypes. The PPAR-α agonists, mainly fibrates (including newer molecules such as pemafibrate) and omega-3 fatty acids, are powerful TG-lowering agents. They mainly affect TG catabolism and, particularly with fibrates, raise the levels of high-density lipoprotein cholesterol (HDL-C). PPAR-γ agonists, mainly glitazones, show a smaller activity on TGs but are powerful glucose-lowering agents. Newer PPAR-α/δ agonists, e.g., elafibranor, have been designed to achieve single drugs with TG-lowering and HDL-C-raising effects, in addition to the insulin-sensitizing and antihyperglycemic effects of glitazones. They also hold promise for the treatment of non-alcoholic fatty liver disease (NAFLD) which is closely associated with the MetS. The PPAR system thus offers an important hope in the management of atherogenic dyslipidemias, although concerns regarding potential adverse events such as the rise of plasma creatinine, gallstone formation, drug-drug interactions (i.
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CAS 848259-27-8 Pemafibrate

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