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-Galphas 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[1].
Molecular Weight:
528.96
Formula:
C21H23ClF2N6O4S
Target:
GABA Receptor,Orphan GPCR,Phosphodiesterase (PDE)
Application Notes:
MCE Product type: Reference compound
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