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Pemafibrate

Catalog No. TQ0107 CAS 848259-27-8

Synonyms: (R)-K-13675

Pemafibrate ((R)-K-13675) is a highly specific PPARα agonist (EC50: 1 nM).

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Pemafibrate, CAS 848259-27-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 51.00
5 mg	In stock	$ 123.00
10 mg	In stock	$ 189.00
25 mg	In stock	$ 369.00
50 mg	In stock	$ 542.00
100 mg	In stock	$ 773.00
1 mL * 10 mM (in DMSO)	In stock	$ 143.00

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Purity: 99.91%

Biological Description

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Description	Pemafibrate ((R)-K-13675) is a highly specific PPARα agonist (EC50: 1 nM).
Targets&IC50	PPARγ (human):1.1 μM (EC50), PPARα (human):1 nM (EC50)
In vitro	Pemafibrate is a potent PPARα agonist, with EC50s of 1 nM, 1.10 μM and 1.58 μM for h-PPARα, h-PPARγ, and h-PPARδ, respectively.
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 significantly reduces the grade of hepatocyte ballooning in PEMA-H mice [2]. Pemafibrate (K-877, 0.0005%) contained in a 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].
Animal Research	Mice are fasted for 12?h and fasting blood glucose measured. Nine-week-old db/db mice are used in the assay. After a 2-week acclimatization period, mice are divided into four groups: BD (db/db) mice (fed basal diet (BD) and treated with 0.5% aqueous methylcellulose solution (MC); MCD (db/db) mice (fed methionine choline-deficient (MCD) and treated with 0.5% MC); PEMA-L (db/db) mice (fed MCD and treated with 0.03?mg/kg Pemafibrate); PEMA-H (db/db) mice (fed MCD and treated with 0.1?mg/kg Pemafibrate). The drug-free solvent or the dosing solution is administered to animals (5?mL/kg body weight, p.o.) once daily (in the morning) for 4 consecutive weeks. After a 2-week acclimatization period, BD mice are fed a BD for 20 weeks. CTRL mice are fed D09100301 for 20 weeks. PEMA-L and PEMA-H mice are fed D09100301 for 12 weeks followed by D09100301 with 0.4?mg and 1.3?mg Pemafibrate/kg of the diet for 8 weeks, which corresponds to 0.03?mg/kg/day and 0.1?mg/kg/day, respectively. FENO mice are fed D09100301 for 12 weeks followed by D09100301 with 666.7?mg fenofibrate/kg of the diet for 8 weeks, which corresponds to 50?mg/kg/day. Pemafibrate and fenofibrate are incorporated into the AMLN diet. Animals are housed under conventional conditions with controlled temperature, humidity, and light (12-h light-dark cycle) and provided with food and water [2].

Synonyms	(R)-K-13675
Molecular Weight	490.55
Formula	C28H30N2O6
CAS No.	848259-27-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 100 mg/mL (203.85 mM)

References and Literature

1. Yamazaki Y, et al. Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4689-93. Epub2007 May 24. 2. Honda Y, et al. Pemafibrate, a novel selective peroxisome proliferator-activated receptor alpha modulator, improves the pathogenesis in a rodent model of nonalcoholic steatohepatitis. Sci Rep. 2017 Feb 14;7:42477. 3. Sairyo M, et al. A Novel Selective PPARα Modulator (SPPARMα), K-877 (Pemafibrate), Attenuates Postprandial Hypertriglyceridemia in Mice. J Atheroscler Thromb. 2018 Feb 1;25(2):142-152.

Citations

1. Matsumoto A, Matsui I, Uchinomiya S, et al.Spatiotemporally quantitative in vivo imaging of mitochondrial fatty acid β-oxidation at cellular-level resolution in mice.American Journal of Physiology-Endocrinology and Metabolism.2023, 325(5): E552-E561.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Hypertension Compound Library Nuclear Receptor Compound Library Bioactive Compound Library Anti-Cardiovascular Disease Compound Library Anti-Diabetic Compound Library Transcription Factor-Targeted Compound Library Anti-Breast Cancer Compound Library

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Keywords

Pemafibrate 848259-27-8 DNA Damage/DNA Repair Metabolism PPAR K13675 K 13675 K-13675 (R)-K-13675 inhibitor inhibit

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