| Identification | Back Directory | [Name]
Pemafibrate | [CAS]
848259-27-8 | [Synonyms]
K877
K-877
CS-2768
Pemafibrate
(R)-K 13675
PEMAFIBRATE;K-877;(R)-K 13675
Butanoic acid, 2-[3-[[2-benzoxazolyl[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]-, (2R)- | [Molecular Formula]
C28H30N2O6 | [MDL Number]
MFCD30533427 | [MOL File]
848259-27-8.mol | [Molecular Weight]
490.55 |
| Chemical Properties | Back Directory | [Melting point ]
98-99 °C(Solv: ethyl acetate (141-78-6); heptane (142-82-5)) | [Boiling point ]
676.7±65.0 °C(Predicted) | [density ]
1.250±0.06 g/cm3(Predicted) | [storage temp. ]
Refrigerator | [solubility ]
Chloroform (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
3.23±0.10(Predicted) | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Uses]
Pemafibrate is used in the treatment of hyperlipidemia. It also functions as a promising selective PPAR-α modulator for treatment of combined dyslipidemia phase 2 clinical trials with K-877. | [in vivo]
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[1]. 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[2]. 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[3]. | [IC 50]
h-PPARα: 1 nM (EC50); h-PPARγ: 1.1 μM (EC50); PPARδ: 1.58 μM (EC50) |
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