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 K_i of 0.21 nM, and mouse K_i 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^[1].

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 (K_i = 0.21 nM) and mouse GPR61 (K_i = 0.72 nM) in overexpressing CHO cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GPR61 Inverse agonist 2 (Compound 15) (10-30 mg/kg; p.o.; twice daily; 14 days) does not alter food intake or body weight in healthy mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

454.88

C₁₈H₁₇ClF₂N₆O₂S

CC1=NC(NS(=O)(C2=C(N=C(C=C2)NCC3=C(C=NC=C3F)F)C)=O)=NC(C)=C1Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Fisher EL, et al. Discovery of Potent and Brain-Penetrant Inverse Agonists for GPR61, an Orphan G Protein-Coupled Receptor. J Med Chem. 2026;69(6):7393-7404.  [Content Brief]