Pemafibrate

Modify Date: 2026-07-02 10:47:49

Pemafibrate Structure
Pemafibrate structure
Common Name Pemafibrate
CAS Number 848259-27-8 Molecular Weight 490.54800
Density N/A Boiling Point N/A
Molecular Formula C28H30N2O6 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Pemafibrate


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, and possesses lipid-lowering effect.

 Names

This table lists Chinese names, IUPAC names and various aliases of this chemical substance.

Name (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid
Synonym More Synonyms

 Pemafibrate Biological Activity

This table contains bioactivity, target information and biological‑assay experimental data of this compound.

Description 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, and possesses lipid-lowering effect.
Related Catalog
Target

h-PPARα:1 nM (EC50)

h-PPARγ:1.1 μM (EC50)

PPARδ:1.58 μM (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. Pemafibrate is more than 1000 fold selective towards PPARα than PPARγ and PPARδ[1].
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].
Animal Admin 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].
References

[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.

 Chemical & Physical Properties

This table shows physicochemical parameters including melting point, boiling point, density, solubility and optical rotation. Missing data is marked as N/A.

Molecular Formula C28H30N2O6
Molecular Weight 490.54800
Exact Mass 490.21000
PSA 94.26000
LogP 5.55410
InChIKey ZHKNLJLMDFQVHJ-RUZDIDTESA-N
SMILES CCC(Oc1cccc(CN(CCCOc2ccc(OC)cc2)c2nc3ccccc3o2)c1)C(=O)O
Storage condition 2-8℃

 PemafibrateBioassay

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This table contains target information, in‑vitro & in‑vivo assay data for this compound.

Name: Diffuse intrinsic pontine glioma (SU-DIPG-XVII) cell line screen of MIPE5.0 library: ...
Source: 15316
Target: N/A
External Id: s-dipg-DIPG17_CTG48h_mipe5_0-1
Name: qHTS drug screen for cell cycle checkpoint inhibitors in PARPi-resistant BRCA-mutant ...
Source: NCGC
External Id: FGL-PARP_PEO-CTG96h-MIPE5.0-p1
Name: Diffuse intrinsic pontine glioma (SU-DIPG-XXV) cell line screen of MIPE5.0 library: v...
Source: 15316
Target: N/A
External Id: s-dipg-DIPG25-MIPE5.0-CTF48h-p1
Name: Cellular viability qHTS for adrenocortical cancer (ACC) cell line SW-13
Source: NCGC
Target: N/A
External Id: ACC-ATC-p1-SW13-72hr
Name: Selectivity for human PPARalpha over PPARgamma
Source: ChEMBL
Target: N/A
External Id: CHEMBL888371
Name: Cellular viability qHTS for adrenocortical cancer (ACC) cell line NCI-H295R
Source: NCGC
Target: N/A
External Id: ACC-ATC-p1-H295R-72hr
Name: Selectivity for human PPARalpha over PPARdelta
Source: ChEMBL
Target: N/A
External Id: CHEMBL888372
Name: Cytotoxicity counterscreen for inhibitors of SARS-CoV-2 cell entry
Source: NCGC
Target: N/A
External Id: TRND-SARS-CoV-2-cytotox-48hr
Name: Diffuse intrinsic pontine glioma (SU-DIPG-XIII) cell line screen of MIPE5.0 library: ...
Source: 15316
Target: N/A
External Id: s-dipg-DIPG13_CTG48h_mipe5_0-1
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 Synonyms

This table collects all English aliases, systematic names and CAS‑related synonyms of the compound.

unii-17vgg92r23
Pemafibrate

 Pemafibrate | FAQ

This section contains frequently‑asked‑questions about this compound, including basic parameters, properties, storage conditions and corresponding answers.

Q: What is the SMILES notation of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid?
A: SMILES notation of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid is CCC(Oc1cccc(CN(CCCOc2ccc(OC)cc2)c2nc3ccccc3o2)c1)C(=O)O.
Q: What is the molecular formula of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid?
A: Molecular formula of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid is C28H30N2O6.
Q: What is the Chinese name of 848259-27-8?
A: Chinese name of 848259-27-8 is Pemafibrate.
Q: What is the English name of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid?
A: The English name of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid is (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid.
Q: What are the uses of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid?
A: Main uses of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid: 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, and possesses lipid-lowering effect.
Q: What English synonyms does (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid have?
A: English synonyms of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid: unii-17vgg92r23, Pemafibrate.
Q: What is the molecular weight of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid?
A: Molecular weight of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid is 490.54800.
Q: What is the LogP of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid?
A: LogP of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid is 5.55410.
Q: What is the CAS number of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid?
A: CAS number of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid is 848259-27-8.
Q: What is the InChIKey of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid?
A: InChIKey of (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid is ZHKNLJLMDFQVHJ-RUZDIDTESA-N.

 Pemafibratefactory

This table lists manufacturers and suppliers of this compound, including vendor names and product supply reference information.

Shanghai Nianxing Industrial Co., Ltd
Dayang Chem (Hangzhou) Co., Ltd.
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