LT175 is a dual ligand targeting peroxisome proliferator-activated receptors alpha and gamma (PPARα/γ). As an orally active partial agonist, it exhibits effective receptor affinity with EC50 values of 0.22 μM for hPPARα, 0.26 μM for mPPARα, and 0.48 μM for hPPARγ. LT175 modulates coregulator recruitment, specifically cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1), via interaction in the hydrophobic "diphenyl pocket" of PPARγ. This compound demonstrates significant insulin-sensitizing effects while reducing adipogenic activity, making it valuable for research in metabolic disorders.
LT175 is a dual ligand targeting peroxisome proliferator-activated receptors alpha and gamma (PPARα/γ). As an orally active partial agonist, it exhibits effective receptor affinity with EC50 values of 0.22 μM for hPPARα, 0.26 μM for mPPARα, and 0.48 μM for hPPARγ. LT175 modulates coregulator recruitment, specifically cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1), via interaction in the hydrophobic "diphenyl pocket" of PPARγ. This compound demonstrates significant insulin-sensitizing effects while reducing adipogenic activity, making it valuable for research in metabolic disorders.
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