Pemafibrateis a selective PPARα modulator (SPPARMα) that has antihyperlipidaemic activity.
pemafibrate 细胞实验
Cell Line
Concentration
Treated Time
Description
References
THP-1 cells
40 or 60 µM
24 hours
To evaluate the effect of pemafibrate on anti-inflammatory macrophage polarization in THP-1 cells. Results showed that pemafibrate promoted anti-inflammatory macrophage polarization and significantly decreased the protein levels of TNF-α and IL-1β.
Sci Rep. 2024 Oct 11;14(1):23816
661W cells
10 and 100 nM
24 hours
To evaluate the inhibitory effect of pemafibrate on HIF activity, results showed no significant inhibitory effect of pemafibrate on HIF activity
Int J Mol Sci. 2019 Nov 23;20(23):5878
Human peritoneal mesothelial cells (HPMCs)
40 or 60 µM
24-48 hours
To investigate the effect of pemafibrate on IFN-γ-induced fibrotic and inflammatory markers in HPMCs. Results showed that pemafibrate effectively inhibited TGF-β1 and fibronectin secretion, stabilized IκBα, and inhibited NF-κB phosphorylation.
Sci Rep. 2024 Oct 11;14(1):23816
Rat aortic smooth muscle cells (RASMCs)
1–1000 nM
48 hours
To evaluate the effect of pemafibrate on VSMC proliferation, results showed that pemafibrate significantly inhibited VSMC proliferation and DNA synthesis.
Heliyon. 2020 Nov 6;6(11):e05431
pemafibrate 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
STZ-induced diabetic model
Diet supplemented
0.0002% pemafibrate
For 12 weeks
To evaluate the protective effect of pemafibrate on diabetic retinopathy, results showed pemafibrate improved blood glucose levels, lipid metabolism, increased serum FGF21 level, and protected retinal neural function
Int J Mol Sci. 2020 Aug 28;21(17):6243
Mice
Nonalcoholic steatohepatitis (NASH) model
Oral
0.03 mg/kg and 0.1 mg/kg
Once daily for 4 weeks
To evaluate the effect of pemafibrate on NASH pathology, results showed that pemafibrate improved obesity, dyslipidaemia, liver dysfunction, and the pathological condition of NASH.
Sci Rep. 2017 Feb 14;7:42477
C57BL/6J mice
STAM mouse model (NASH model)
Oral
0.1 mg/kg
Once daily for 3 weeks
To evaluate the protective effects of pemafibrate against NASH development. Results showed that pemafibrate improved F4/80-positive macrophage accumulation, ballooning degeneration of hepatocytes, and the NAFLD activity score without affecting hepatic triglyceride accumulation.
Sci Rep. 2020 May 8;10(1):7818
C57Bl/6 male mice
Diet-induced steatohepatitis-related cardiomyopathy model
Oral
0.1 mg/kg
Daily administration for 8 weeks
To evaluate the effect of pemafibrate on steatohepatitis and cardiomyopathy. Results showed that pemafibrate significantly suppressed inflammation and fibrosis in the liver and heart, and improved cardiac function.
Sci Rep. 2022 Feb 22;12(1):2996
Balb/c mice
Hepatic ischemia-reperfusion injury (HIRI) model
Intraperitoneal injection
0.1 mg/kg, 0.5 mg/kg, 1.0 mg/kg
Once daily for 5 days
To investigate the role of pemafibrate in hepatic ischemia-reperfusion injury, the results showed that pemafibrate effectively reduced the level of hepatic IR injury. Additionally, pemafibrate exhibited anti-inflammatory, antiapoptotic, and antiautophagy effects, mediated by the JAK2/STAT3β/PPARα pathway.
PPAR Res. 2021 Mar 11;2021:6632137
C57BL/6 mice
Vascular injury model in mice fed a high-fat diet (HFD) or normal chow
Oral
0.1 mg/kg/day
Once daily for 6 weeks
To evaluate the effect of pemafibrate on neointima formation after vascular injury, results showed that pemafibrate significantly reduced neointima formation and VSMC proliferation.
Heliyon. 2020 Nov 6;6(11):e05431
Human
Type 2 diabetes patients with hypertriglyceridemia
Oral
0.2 mg (0.1 mg twice daily)
Twice daily for 24 weeks
To evaluate the effects of pemafibrate on serum lipids in type 2 diabetes patients with hypertriglyceridemia. Results showed that pemafibrate significantly reduced serum TGs, midband and VLDL fractions, but LDL-C levels increased depending on baseline TGs and LDL-C levels.
Lipids Health Dis. 2021 Feb 20;20(1):17
Human
Patients with type 2 diabetes and hypertriglyceridemia
Oral
0.2–0.4 mg/day
Once daily for 52 weeks
To evaluate the effect of pemafibrate on insulin resistance and β-cell function. Results showed that pemafibrate significantly improved insulin resistance assessed by HOMA2-R and maintained β-cell function assessed by disposition index.
Pharmaceutics. 2023 Jun 27;15(7):1838
Human
Patients with type 2 diabetes and hypertriglyceridemia
Oral
0.2–0.4 mg/day
Once daily for 52 weeks
To evaluate the effects of pemafibrate on metabolic-associated fatty liver disease (MAFLD), results showed pemafibrate significantly improved ALT levels and liver fibrosis in subjects with higher ALT levels.
Diabetol Metab Syndr. 2023 Oct 26;15(1):214
C57BL/6J mice
MGO-induced peritoneal fibrosis model
Oral
0.3 mg/kg/day
Once daily for 3 weeks
To evaluate the effect of pemafibrate on MGO-induced peritoneal fibrosis and inflammation. Results showed that pemafibrate significantly reduced peritoneal fibrosis and inflammatory markers, restored peritoneal function, and promoted anti-inflammatory macrophage polarization.
Sci Rep. 2024 Oct 11;14(1):23816
C57BL/6J mice
Oxygen-induced retinopathy (OIR) model
Oral gavage
0.3 mg/kg/day
Daily from P12 to P16
To evaluate the inhibitory effect of pemafibrate on retinal pathological neovascularization, results showed pemafibrate significantly reduced pathological angiogenesis
Int J Mol Sci. 2019 Nov 23;20(23):5878
Mice
Fatty acid overload nephropathy model
Oral gavage
0.5 mg/kg/day
Once daily for 20 days
To evaluate the protective effect of PEM against FAON, results showed that PEM significantly attenuated tubular injury caused by FAON, increased the expressions of mRNA and proteins related to FAM, and decreased renal FFA content and oxidative stress.
Metabolites. 2021 Jun 9;11(6):372
Dahl salt-sensitive rats
Hypertension and insulin resistance model
Oral gavage
0.5 mg/kg/day
Once daily for 12 weeks
To assess the effect of combination therapy on lipid profiles and endothelial dysfunction. Combination therapy significantly reduced systolic blood pressure, TG levels (including total TG, CM-TG, VLDL-TG, HDL-TG), and cholesterol levels (including total cholesterol, CM-cholesterol, VLDL-cholesterol, LDL-cholesterol), and improved endothelium-dependent vascular relaxation.
Cardiovasc Diabetol. 2020 Sep 26;19(1):149
C57BL/6 mice
Unilateral common carotid artery occlusion (UCCAO)-induced retinal ischemia model
Oral
0.5 mg/kg/day
Once daily for 4 days before UCCAO surgery, then continuously administered until the end of experiments
To evaluate the protective effects of pemafibrate against UCCAO-induced retinal dysfunction. Results showed that pemafibrate enhanced liver function, elevated serum FGF21 levels, protected retinal function, modulated retinal gliosis, and preserved oscillatory potentials.
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