GPR61 Inverse agonist 2
GPR61 Inverse agonist 2 is a selective GPR61 inverse agonist with human IC50 of 6.2 nM and mouse IC50 of 20 nM, human Ki of 0.21 nM, and mouse Ki of 0.72 nM. GPR61 Inverse agonist 2 binds to an induced intracellular allosteric pocket of GPR61, disrupts receptor-Gαs interactions, and abolishes GPR61 constitutive activity. GPR61 Inverse agonist 2 does not alter food intake or body weight in healthy mice. GPR61 Inverse agonist 2 can be used for the research of cachexia/sarcopenia.
For research use only. We do not sell to patients.
- Formula: C18H17ClF2N6O2S
- Molecular Weight:454.88
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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
GPR61 Inverse agonist 2 (Compound 15) potently inhibits constitutive activity of human GPR61 in overexpressing CHO cells with an IC50 of 6.2 nM[1].
GPR61 Inverse agonist 2 inhibits constitutive activity of mouse GPR61 in overexpressing cells with an IC50 of 20 nM[1].
GPR61 Inverse agonist 2 engages specifically with human GPR61 to increase receptor cell surface expression and suppress constitutive activity, with no activity against MC4R[1].
GPR61 Inverse agonist 2 binds specifically to human GPR61-overexpressing CHO cells, with no significant binding to parental CHO cells[1].
GPR61 Inverse agonist 2 binds with high affinity to human GPR61 (Ki = 0.21 nM) and mouse GPR61 (Ki = 0.72 nM) in overexpressing CHO cells[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 weeks old)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; twice daily; 14 days
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Result:Showed no statistically significant changes in food intake over 14 days.
Showed no statistically significant changes in body weight over 14 days.
Chemical Information
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Molecular Weight 454.88
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Formula C18H17ClF2N6O2S
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SMILES
CC1=NC(NS(=O)(C2=C(N=C(C=C2)NCC3=C(C=NC=C3F)F)C)=O)=NC(C)=C1Cl
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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 2 Related Classifications
HY-182270 Related Classifications
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