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LT175 

Cat. No. M30723
LT175  Structure
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Biological Activity

LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC50=0.22 μm; mPPARα:EC50=0.26 μm; hPPARγ:EC50=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties.

Chemical Information
Molecular Weight 318.37
Formula C21H18O3
CAS Number 862901-87-9
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Hiroyuki Kojima, et al. J Med Chem. Covalent Modifier Discovery Using Hydrogen/Deuterium Exchange-Mass Spectrometry

[2] Antonio Laghezza, et al. J Med Chem. A New Antidiabetic Agent Showing Short- and Long-Term Effects Due to Peroxisome Proliferator-Activated Receptor Alpha/Gamma Dual Agonism and Mitochondrial Pyruvate Carrier Inhibition

[3] Luca Piemontese, et al. Eur J Med Chem. Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175

[4] Clorinda Lori, et al. Acta Crystallogr D Biol Crystallogr. Structural basis of the transactivation deficiency of the human PPARγ F360L mutant associated with familial partial lipodystrophy

[5] Federica Gilardi, et al. J Biol Chem. LT175 is a novel PPARα/γ ligand with potent insulin-sensitizing effects and reduced adipogenic properties

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Keywords: LT175  supplier, PPAR, inhibitors, activators


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