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Pemafibrate

Cat. No. M10245
Pemafibrate Structure
Synonym:

K-877; (R)-K 13675; CS-2768

Size Price Availability Quantity
5mg USD 280  USD280 In stock
10mg USD 360  USD360 In stock
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Quality Control & Documentation
Biological Activity

Pemafibrate is a potent and highly specific PPARα agonist, with EC50s of 1 nM, 1.10 μM and 1.58 μM for h-PPARα, h-PPARγ and h-PPARδ, respectively. Pemafibrate (0.03 mg/kg) decreases levels of triglycerides and aspartate aminotransferase (AST) in PEMA-L (db/db) mice. 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.

Chemical Information
Molecular Weight 490.55
Formula C28H30N2O6
CAS Number 848259-27-8
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Masami Sairyo, et al. J Atheroscler Thromb. A Novel Selective PPARα Modulator (SPPARMα), K-877 (Pemafibrate), Attenuates Postprandial Hypertriglyceridemia in Mice

[2] Yasushi Honda, et al. Sci Rep. Pemafibrate, a novel selective peroxisome proliferator-activated receptor alpha modulator, improves the pathogenesis in a rodent model of nonalcoholic steatohepatitis

[3] Yukiyoshi Yamazaki, et al. Bioorg Med Chem Lett. Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists

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Keywords: Pemafibrate, K-877; (R)-K 13675; CS-2768 supplier, PPAR, inhibitors, activators


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