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MA-0204

Cat. No. M10513
MA-0204 Structure
Synonym:

CS-2841; MA0204

Size Price Availability Quantity
5mg USD 420  USD420 In stock
10mg USD 710  USD710 In stock
25mg USD 1300  USD1300 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

MA-0204 is a highly potent and selective PPARδ modulator (PPARδ EC50 = 0.4 nM; PPARα, EC50 = 6,660 nM) that upregulates the expression of FAO genes in human renal proximal tubule cells, resulting in increased mitochondrial fatty acid oxidation. MA-0204 is >10,000-fold selective for activation of PPARδ over PPARα and PPARγ receptors. MA-0204 exhibits high protein binding to mouse plasma, good permeability and low potential for efflux. C.

In normal rats undergoing IR-AKI, MA-0204 attenuates the increases of plasma and urinary biomarkers of AKI, improves renal function, mitigates proximal tubular damage and boosts mitochondrial gene expression. PPARδ (30, 100 mg/kg) increases target gene transcription in the muscle.

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 476.49
Formula C25H27F3N2O4
CAS Number 2095128-17-7
Purity >99%
Solubility DMSO 39 mg/mL
Storage at -20°C
References

[1] Bharat Lagu, et al. ACS Med Chem Lett. Selective PPARδ Modulators Improve Mitochondrial Function: Potential Treatment for Duchenne Muscular Dystrophy (DMD)

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MA-0204, CS-2841; MA0204 supplier, PPAR, inhibitors

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