Pemafibrate
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MedKoo CAT#: 206448

CAS#: 848259-27-8 (free acid)

Description: Pemafibrate, also known as (R)-K 13675, is a PPAR alpha agonist. (R)-K-13675 decreases the secretion of inflammatory markers without affecting cell proliferation or tube formation. Peroxisome proliferator-activated receptor-alpha (PPAR-alpha) is a key regulator of lipid and glucose metabolism and has been implicated in inflammation. (R)-K-13675 was associated with the inhibition of inflammatory responses without affecting cell proliferation or angiogenesis, and subsequently may induce an anti-atherosclerotic effect.

Chemical Structure

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Pemafibrate
CAS# 848259-27-8 (free acid)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206448
Name: Pemafibrate
CAS#: 848259-27-8 (free acid)
Chemical Formula: C28H30N2O6
Exact Mass: 490.21
Molecular Weight: 490.560
Elemental Analysis: C, 68.56; H, 6.16; N, 5.71; O, 19.57

Price and Availability

Size Price Availability Quantity
5mg USD 150 Ready to ship
10mg USD 250 Ready to ship
25mg USD 550 Ready to ship
50mg USD 950 Ready to ship
100mg USD 1650 Ready to ship
200mg USD 2650 Ready to Ship
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Related CAS #: 950644-31-2 (sodium)   848259-27-8 (free acid)  

Synonym: K-877; K877; K 877; (R)-K 13675; (R)-K13675; (R)K-13675; Pemafibrate

IUPAC/Chemical Name: (R)-2-(3-((benzo[d]oxazol-2-yl(3-(4-methoxyphenoxy)propyl)amino)methyl)phenoxy)butanoic acid

InChi Key: ZHKNLJLMDFQVHJ-RUZDIDTESA-N

InChi Code: InChI=1S/C28H30N2O6/c1-3-25(27(31)32)35-23-9-6-8-20(18-23)19-30(28-29-24-10-4-5-11-26(24)36-28)16-7-17-34-22-14-12-21(33-2)13-15-22/h4-6,8-15,18,25H,3,7,16-17,19H2,1-2H3,(H,31,32)/t25-/m1/s1

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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: Pemafibrate is a selective antagonist of peroxisome proliferator-activated receptor α (PPARα; EC50 = 1 nM for transcriptional activity), a transcription factor that is essential for regulation of lipid homostasis, and is selective for PPARα over PPARδ and PPARγ (EC50 = 2,300 and 1,000 nM, respectively, for transcriptional activity).
In vitro activity: Under HG + H/R conditions, NF-κB protein expression levels were significantly enhanced in H9c2 cells compared with those in the control group (P<0.001; Fig. 4A). Pemafibrate significantly suppressed the protein expression levels of NF-κB compared with those in the HG + H/R group (P<0.001; Fig. 4A). To evaluate whether pemafibrate may regulate mitochondrial dysfunction and apoptosis through the NF-κB signaling pathway, NF-κB was overexpressed in H9c2 cells (P<0.001; Fig. 4B). The results demonstrated that overexpression of NF-κB reversed the pemafibrate-induced increase in ATP levels in the HG + H/R treatment group (P<0.01 vs. pemafibrate + HG + H/R and pemafibrate + HG + H/R + NC; Fig. 4C). Pemafibrate decreased the expression levels of cleavedcaspase-3 compared with those in the HG + H/R group; however, overexpression of NF-κB reversed this effect (P<0.01 vs. pemafibrate + HG + H/R and pemafibrate + HG + H/R + NC; Fig. 4D), indicating that pemafibrate inhibited the HG + H/R-induced apoptosis by regulating the NF-κB signaling pathway. However, overexpression of NF-κB expression failed to significantly reverse the pemafibrate-induced reduction in Cyt-c expression levels (Fig. 4D). These results suggest that pemafibrate may prevent mitochondrial dysfunction by interacting with the NF-κB signaling pathway. Exp Ther Med. 2021 Apr; 21(4): 331. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7903427/
In vivo activity: To verify the effect of pemafibrate on STAM mouse livers, a comprehensive transcriptome analysis was performed by RNA-seq using liver tissues collected from normal, STAM control, and pemafibrate-treated STAM mice. 187 up-regulated and 477 down-regulated genes were identified in the pemafibrate-treated compared with the STAM control group by our stringent criteria (Supplementary Table 1). In fact, PPARα–regulated FAO-related genes were significantly induced in the pemafibrate-treated group (Supplementary Fig. 1). The expression levels of genes related to TG hydrolysis, fatty acid uptake, fatty acid activation, fatty acid binding, peroxisomal and mitochondrial oxidation, and ketogenesis were higher in the STAM control group than in the normal group (Supplementary Figs. 1 and 2). Pemafibrate apparently induced the expression of these genes. In particular, pemafibrate treatment resulted in the greatest increase in Pdk4 expression, suggesting that it mediates the suppression of glucose oxidation and preferential activation of fatty acid oxidation (Supplementary Figs. 1 and 2). Pemafibrate did not influence glycolysis and Pck1 expression but significantly induced a series of genes involved in TG synthesis from DHAP and glycerol (Fig. 2E,F). Pemafibrate had the greatest effect on Mogat1, which has key roles in TG re-esterification from monoacylglycerols and diacylglycerols generated by TG hydrolysis24 in STAM mouse livers (Fig. 2E,F). These results suggest that pemafibrate enhances TG synthesis from DHAP and glycerol and the re-esterification of glycerol generated by TG hydrolysis in STAM mouse livers. Sci Rep. 2020; 10: 7818. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7210999/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 30.0 61.20

Preparing Stock Solutions

The following data is based on the product molecular weight 490.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Li W, Xu J, Guo X, Xia X, Sun Y. Pemafibrate suppresses oxidative stress and apoptosis under cardiomyocyte ischemiareperfusion injury in type 1 diabetes mellitus. Exp Ther Med. 2021 Apr;21(4):331. doi: 10.3892/etm.2021.9762. Epub 2021 Feb 8. PMID: 33732304; PMCID: PMC7903427. 2. Horikawa T, Kawanami T, Hamaguchi Y, Tanaka Y, Kita S, Ryorin R, Takashi Y, Takahashi H, Tanabe M, Yanase T, Kawanami D, Nomiyama T. Pemafibrate, a PPAR alpha agonist, attenuates neointima formation after vascular injury in mice fed normal chow and a high-fat diet. Heliyon. 2020 Nov 6;6(11):e05431. doi: 10.1016/j.heliyon.2020.e05431. PMID: 33204884; PMCID: PMC7653074. 3. Sasaki Y, Asahiyama M, Tanaka T, Yamamoto S, Murakami K, Kamiya W, Matsumura Y, Osawa T, Anai M, Fruchart JC, Aburatani H, Sakai J, Kodama T. Pemafibrate, a selective PPARα modulator, prevents non-alcoholic steatohepatitis development without reducing the hepatic triglyceride content. Sci Rep. 2020 May 8;10(1):7818. doi: 10.1038/s41598-020-64902-8. PMID: 32385406; PMCID: PMC7210999. 4. Tomita Y, Ozawa N, Miwa Y, Ishida A, Ohta M, Tsubota K, Kurihara T. Pemafibrate Prevents Retinal Pathological Neovascularization by Increasing FGF21 Level in a Murine Oxygen-Induced Retinopathy Model. Int J Mol Sci. 2019 Nov 23;20(23):5878. doi: 10.3390/ijms20235878. PMID: 31771164; PMCID: PMC6928689
In vitro protocol: 1. Li W, Xu J, Guo X, Xia X, Sun Y. Pemafibrate suppresses oxidative stress and apoptosis under cardiomyocyte ischemiareperfusion injury in type 1 diabetes mellitus. Exp Ther Med. 2021 Apr;21(4):331. doi: 10.3892/etm.2021.9762. Epub 2021 Feb 8. PMID: 33732304; PMCID: PMC7903427. 2. Horikawa T, Kawanami T, Hamaguchi Y, Tanaka Y, Kita S, Ryorin R, Takashi Y, Takahashi H, Tanabe M, Yanase T, Kawanami D, Nomiyama T. Pemafibrate, a PPAR alpha agonist, attenuates neointima formation after vascular injury in mice fed normal chow and a high-fat diet. Heliyon. 2020 Nov 6;6(11):e05431. doi: 10.1016/j.heliyon.2020.e05431. PMID: 33204884; PMCID: PMC7653074.
In vivo protocol: 1. Sasaki Y, Asahiyama M, Tanaka T, Yamamoto S, Murakami K, Kamiya W, Matsumura Y, Osawa T, Anai M, Fruchart JC, Aburatani H, Sakai J, Kodama T. Pemafibrate, a selective PPARα modulator, prevents non-alcoholic steatohepatitis development without reducing the hepatic triglyceride content. Sci Rep. 2020 May 8;10(1):7818. doi: 10.1038/s41598-020-64902-8. PMID: 32385406; PMCID: PMC7210999. 2. Tomita Y, Ozawa N, Miwa Y, Ishida A, Ohta M, Tsubota K, Kurihara T. Pemafibrate Prevents Retinal Pathological Neovascularization by Increasing FGF21 Level in a Murine Oxygen-Induced Retinopathy Model. Int J Mol Sci. 2019 Nov 23;20(23):5878. doi: 10.3390/ijms20235878. PMID: 31771164; PMCID: PMC6928689

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