Orphan GPCR Inhibitor

AF64394 is a GPR3 inverse agonist, with a pIC₅₀ of 7.3.

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 K_i of 0.34 nM, mouse K_i of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABA_A 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 1 (Compound 1) is a GPR61 inverse agonist (IC₅₀: 11 nM). GPR61 Inverse agonist 1 can be used for research of disorders of metabolism and body weight, such as obesity and cachexia.

Gue1654 is a modulator of OXE-R. Gue1654 inhibits Gβγ but not Gα signaling triggered upon activation of Gα(i)-βγ by the chemoattractant receptor OXE-R. Gue1654 does not interfere nonspecifically with signaling directly at or downstream of Gβγ.

Vemzatatug is a humanized IgG1κ monoclonal antibody inhibitor targeting GPRC5D. Vemzatatug has an antitumor activity. Vemzatatug can be used for cancers like multiple myeloma (MM) research.

SAR-446523 is a humanized IgG1 monoclonal antibody inhibitor targeting GPRC5D. SAR-446523 significantly induces antibody-dependent cell-mediated cytotoxicity (ADCC). SAR-446523 has potent antitumor activity with improvement of mouse survival in NK humanized NOG huIL15 transgenic mice model bearing MM cells. SAR-446523 can be used for multiple myeloma (MM) research.

Anti-Mouse F4/80 Antibody (Cl:A3-1) reacts with the mouse F4/80. The F4/80 receptor is generally considered a murine pan-macrophage marker. Recommend Isotype Controls: Rat IgG2b kappa, Isotype Control (HY-P990682).

PSB-CB-27 is a potent and selective GPR18 inhibitor with an IC₅₀ of 0.65 μM. PSB-CB-27 shows selectivity over Human GPR55, Human CB1 receptor, and Human CB2 receptor. PSB-CB-27 leads to a complete blockade of Δ9-Tetrahydrocannabinol (THC)-induced GPR18 activation. PSB-CB-27 can be used for inflammatory diseases and cancer immunotherapy research.