GPR61 Inverse agonist 3
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.
For research use only. We do not sell to patients.
- Formula: C21H23ClF2N6O4S
- Molecular Weight:528.96
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PDE3A 8.9 μM () |
GPR61 Inverse agonist 3 (Compound 23) potently inhibits constitutive activity of human GPR61 in TREx-inducible overexpressed CHO cells with an IC50 of 4.0 nM and binds human GPR61 with a Ki of 0.34 nM[1].
GPR61 Inverse agonist 3 potently inhibits constitutive activity of mouse GPR61 in overexpressed CHO cells with an IC50 of 8.8 nM and binds mouse GPR61 with a Ki of 1.1 nM[1].
GPR61 Inverse agonist 3 has moderate MDR1 efflux, low BCRP efflux, good passive permeability, and high intrinsic clearance in human hepatocytes, with respective values of 7.4, 1.2, 32 × 10-6 cm/s, and 152 μL/min/million cells[1].
GPR61 Inverse agonist 3 (10 μM) is highly selective for GPR61, with only moderate off-target activity against the GABAA chloride channel (IC50 = 4.6 μM) and PDE3A1 (IC50 = 8.9 μM), and no significant activity against 104 other targets or tested ion channels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice (10-11 week-old)[1]
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Dosage:300 mg/kg
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Administration:p.o.; single dose (administered 2 h after ABT pretreatment)
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Result:Did not produce a statistically significant increase in 24-hour cumulative food intake compared to vehicle controls.
Chemical Information
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Molecular Weight 528.96
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Formula C21H23ClF2N6O4S
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SMILES
COCCN(S(=O)(C1=CC=C(N=C1OC)NCC2=C(C=NC=C2F)F)=O)C3=NC(C)=C(C(C)=N3)Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GPR61 Inverse agonist 3 Related Classifications
HY-182271 Related Classifications
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