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GPR61 Inverse agonist 3

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-182271

    Orphan GPCR GABA Receptor Phosphodiesterase (PDE) Metabolic Disease
    GPR61 Inverse agonist 3 is a selective and brain-penetrant GPR61 inverse agonist with human IC50 of 4.0 nM, mouse IC50 of 8.8 nM, human Ki of 0.34 nM, mouse Ki of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABAA chloride channel and PDE3A1 with IC50 values of 4.6 and 8.9 μM. GPR61 Inverse agonist 3 shows no functional effect on food intake in adult mice co-administered with a pan-CYP inhibitor. GPR61 Inverse agonist 3 can be used for the research of cachexia/sarcopenia .
    GPR61 Inverse agonist 3

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