Description
Pemafibrate is a potent PPARα agonist, with EC50s of 1 nM, 1.10 uM and 1.58 uM for h-PPARα, h-PPARγ and h-PPARδ, respectively, and possesses lipid-lowering effect. Pemafibrate is a potent PPARα agonist, with EC50s of 1 nM, 1.10 uM and 1.58 uM for h-PPARα, h-PPARγ and h-PPARδ, respectively. Pemafibrate is more than 1000 fold selective towards PPARα than PPARγ and PPARδ. Pemafibrate (3 mg/kg, p.o.) increases plasma h-apoA-I in human apoA-I (h-apoA-I) transgenic mice, and shows higher levels of plasma h-apoA-I than fenofibrate at 300 mg/kg. Pemafibrate (0.03 mg/kg) decreases levels of triglycerides and aspartate aminotransferase (AST) in PEMA-L (db/db) mice. Pemafibrate (0.1 mg/kg) not only shows such effects but increases liver weight in PEMA-H (db/db) mice. Pemafibrate enhances the pathogenesis in a rodent model of nonalcoholic steatohepatitis (NASH). Pemafibrate significantlly reduces the grade of hepatocyte ballooning in PEMA-H mice. Furthermore, Pemafibrate modulates lipid turnover and induces uncoupling protein 3 (UCP 3) expression in the liver. Pemafibrate (K-877, 0.0005%) contained in high-fat diet (HFD) inhibits the body weight gain in mice. Pemafibrate significantly decreases the abundance of triglyceride (TG)-rich lipoproteins, including remnants, in postprandial plasma of mice. Pemafibrate also decreases intestinal mRNA expression of ApoB and Npc1l1.
Product information
CAS Number: 848259-27-8
Molecular Weight: 490.55
Formula: C28H30N2O6
Chemical Name: (2R)-2-(3-{[(1,3-benzoxazol-2-yl)[3-(4-methoxyphenoxy)propyl]amino]methyl}phenoxy)butanoic acid
Smiles: COC1C=CC(=CC=1)OCCCN(CC1C=CC=C(C=1)O[C@H](CC)C(O)=O)C1=NC2=CC=CC=C2O1
InChiKey: ZHKNLJLMDFQVHJ-RUZDIDTESA-N
InChi: InChI=1S/C28H30N2O6/c1-3-25(27(31)32)35-23-9-6-8-20(18-23)19-30(28-29-24-10-4-5-11-26(24)36-28)16-7-17-34-22-14-12-21(33-2)13-15-22/h4-6,8-15,18,25H,3,7,16-17,19H2,1-2H3,(H,31,32)/t25-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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