Referencia número: HY-17618

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Pemafibrate

(Synonyms: (R)-K-13675)

10 Cited Publications

Revisión del cliente

Based on 10 publication(s) in Google Scholar

Pemafibrate is a highly selective PPARα agonist, with an EC₅₀ of 1 nM.

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Pureza: 99.85%
No. CAS: 848259-27-8
Fòrmula: C₂₈H₃₀N₂O₆
Peso molecular:490.55

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Pemafibrate Chemical Structure

No. CAS: 848259-27-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (10)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Pemafibrate is a highly selective PPARα agonist, with an EC₅₀ of 1 nM.

IC₅₀ & Target^[1]

h-PPARα

1 nM (EC₅₀)

h-PPARγ

1.1 μM (EC₅₀)

PPARδ

1.58 μM (EC₅₀)

Ver todos los productos específicos de isoformas PPAR :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	EC₅₀	1 nM Compound: SC-3	Agonist activity at GAL4-tagged PPARalpha ligand-binding domain (unknown origin) expressed in HEK293T cells incubated for 16 to 19 hrs by beta-lactamase reporter gene assay Agonist activity at GAL4-tagged PPARalpha ligand-binding domain (unknown origin) expressed in HEK293T cells incubated for 16 to 19 hrs by beta-lactamase reporter gene assay	[PMID: 25491112]

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. Pemafibrate is more than 1000 fold selective towards PPARα than PPARγ and PPARδ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 848259-27-8
Appearance Solid
Peso molecular 490.55
Fòrmula C₂₈H₃₀N₂O₆
Color White to off-white
SMILES

CC[C@@H](OC1=CC=CC(CN(C2=NC3=CC=CC=C3O2)CCCOC4=CC=C(OC)C=C4)=C1)C(O)=O
Synonyms

(R)-K-13675
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (10)

All Cell Proliferation/Viability AssayWBIFRT-PCR

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Journal Impact Factor

J Clin Invest

Endothelial lipid droplets suppress eNOS to link high fat consumption to blood pressure elevation. [Abstract]

2023 Dec 15;133(24):e173160. PMID: 37824206
Cell Biol Toxicol

Human hepatic in vitro models reveal distinct anti-NASH potencies of PPAR agonists. [Abstract]

2021 Apr;37(2):293-311. PMID: 32613381

Pemafibrate purchased from MedChemExpress. Usage Cited in: Cell Biol Toxicol. 2021 Apr;37(2):293-311. [Abstract]

a ATP content in NASH-triggered hSKP-HPC upon increasing concentrations of PPAR agonists (Pemafibrate; 60, 100, 200 μM; 24 h). b ATP content in NASH-triggered HepG2, HepaRG and PHH cultures upon exposure to PPAR agonists at a concentration of 60 µM.

Pemafibrate purchased from MedChemExpress. Usage Cited in: Cell Biol Toxicol. 2021 Apr;37(2):293-311. [Abstract]

Pemafibrate (60 μM) reduces lipid levels only in HepG2 and PHH. Micrographs of in vitro NASH models stained for neutral lipids with BODIPY™ 493/503 (green) and DAPI (blue, nuclei).

Pemafibrate purchased from MedChemExpress. Usage Cited in: Cell Biol Toxicol. 2021 Apr;37(2):293-311. [Abstract]

Pemafibrate (10 μM) decreased the ACTA2 and COL1A1 mRNA level, increased the LOXL2 mRNA levels in human LX-2 stellate cells.
Int J Neuropsychopharmacol

Pemafibrate treatment produces antidepressant-like effects in CUMS and CRS models through activation of hippocampal PPARa and BDNF signaling. [Abstract]

2025 Aug 30:pyaf063. PMID: 40884470
Drug Metab Dispos

Metabolic flux analysis of bile acid biosynthesis acidic pathway in HepG2 cells reveals CYP8B1 inhibition of azole antifungals. [Abstract]

2025 Nov;53(11):100168. PMID: 41124962
PPAR Res

Pemafibrate Pretreatment Attenuates Apoptosis and Autophagy during Hepatic Ischemia-Reperfusion Injury by Modulating JAK2/STAT3 β/PPAR α Pathway. [Abstract]

2021 Mar 11:2021:6632137. PMID: 33777128
Open Biol

Identification of a novel regulatory pathway for PPARα by RNA-seq characterization of the endothelial cell lipid peroxidative injury transcriptome. [Abstract]

2019 Dec;9(12):190141. PMID: 31847785

Pemafibrate purchased from MedChemExpress. Usage Cited in: Open Biol. 2019 Dec;9(12):190141. [Abstract]

Pemafibrate increased the protein expression of CCL2 in stable CCL2 knockdown HUVECs.

Pemafibrate purchased from MedChemExpress. Usage Cited in: Open Biol. 2019 Dec;9(12):190141. [Abstract]

Pemafibrate did not inhibit HUVEC apoptosis when CCL2 expression was inhibited.
Life Sci Alliance

Sex-regulated gene dosage effect of PPARα on synaptic plasticity. [Abstract]

2019 Mar 20;2(2):e201800262. PMID: 30894406
Biochem Biophys Res Commun

Pemafibrate, a selective PPARα modulator, and fenofibrate suppress microglial activation through distinct PPARα and SIRT1-dependent pathways. [Abstract]

2020 Apr 2;524(2):385-391. PMID: 32005522
Exp Ther Med

Pemafibrate suppresses oxidative stress and apoptosis under cardiomyocyte ischemia-reperfusion injury in type 1 diabetes mellitus. [Abstract]

2021 Apr;21(4):331. PMID: 33732304
Research Square Preprint

2021 Sep.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (203.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0385 mL

10.1926 mL

20.3853 mL

5 mM

0.4077 mL

2.0385 mL

4.0771 mL

10 mM

0.2039 mL

1.0193 mL

2.0385 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.10 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

Animal Administration^[2]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (278 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0385 mL	10.1926 mL	20.3853 mL	50.9632 mL
	5 mM	0.4077 mL	2.0385 mL	4.0771 mL	10.1926 mL
	10 mM	0.2039 mL	1.0193 mL	2.0385 mL	5.0963 mL
	15 mM	0.1359 mL	0.6795 mL	1.3590 mL	3.3975 mL
	20 mM	0.1019 mL	0.5096 mL	1.0193 mL	2.5482 mL
	25 mM	0.0815 mL	0.4077 mL	0.8154 mL	2.0385 mL
	30 mM	0.0680 mL	0.3398 mL	0.6795 mL	1.6988 mL
	40 mM	0.0510 mL	0.2548 mL	0.5096 mL	1.2741 mL
	50 mM	0.0408 mL	0.2039 mL	0.4077 mL	1.0193 mL
	60 mM	0.0340 mL	0.1699 mL	0.3398 mL	0.8494 mL
	80 mM	0.0255 mL	0.1274 mL	0.2548 mL	0.6370 mL
	100 mM	0.0204 mL	0.1019 mL	0.2039 mL	0.5096 mL

Keywords

Pemafibrate

10 Cited Publications

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Pemafibrate

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Publications Citing Use of MedChemExpress (MCE) Pemafibrate

Ver todos los productos específicos de isoformas PPAR

Actividad biológica

Chemical Information

Publications (10)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Pemafibrate Related Classifications

HY-17618 Related Classifications