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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
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 490.55
Formula C28H30N2O6
CAS Number 848259-27-8
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
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

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