GPR39 Agonist

Lithocholic acid 3-sulfate disodium is a GPR39 agonist, with EC₅₀ values of 41 μM and 42.4 μM in M39-20 and hGPR39-2 cells, respectively, in the absence of Zn²⁺, and 0.88 μM and 0.97 μM in the presence of Zn²⁺. Lithocholic acid 3-sulfate disodium acts as a RORγt ligand. Lithocholic acid 3-sulfate disodium stimulates the GPR39 receptor to initiate intracellular calcium signaling, independent of the Zn²⁺-binding sites H17 and H19. LCA-3-S selectively inhibits Th17 cell differentiation by targeting RORγt. Lithocholic acid 3-sulfate disodium can be used in the research of cholestatic liver diseases.

TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC₅₀ values of 0.4 and 0.8 nM for rat and human receptors respectively.

Taurolithocholic acid 3-sulfate disodium is a GPR39 agonist with EC₅₀s of 71.6  and 69.4 (absence of Zn²⁺) and 9 and 9.6 μM (presence of Zn²⁺) in M39-20 and hGPR39-2 cells, respectively. Taurolithocholic acid 3-sulfate disodium stimulates GPR39 receptors to initiate intracellular calcium signaling, independent of Zn²⁺ binding sites H17 and H19. Taurolithocholic acid 3-sulfate disodium can be used for the research of gallbladder disease.

TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC₅₀s of 9 nM/5 nM in the presence of Zn²⁺, and 280 nM/180 nM in the absence of Zn²⁺ for human/murine GPR39.

Glycolithocholic acid 3-sulfate disodium is a GPR39 agonist with EC₅₀s of 47.9  and 66.8 μM (absence of Zn²⁺) and 8 and 8.7 μM (presence of Zn²⁺) in M39-20 and hGPR39-2 cells, respectively. Glycolithocholic acid 3-sulfate disodium stimulates GPR39 receptors to initiate intracellular calcium signaling, independent of Zn²⁺ binding sites H17 and H19. Glycolithocholic acid 3-sulfate disodium also inhibits replication of HIV-1 in vitro. Glycolithocholic acid 3-sulfate disodium can be used for the research of HIV infection and gallbladder disease.

TMN-OMe is a blood-brain barrier-permeable GPR39 agonist and a radiotracer for positron emission tomography (PET). TMN-OMe activates GPR39 by recruiting β-arrestin, exhibits highly selective binding ability in the mouse brain, and enables quantitative analysis of GPR39 at the in vivo level. TMN-OMe shows specific uptake in GPR39 knockout mice, Alzheimer's disease model (APP/PS1) mice, and blocking experiments. TMN-OMe facilitates in-depth exploration of changes in GPR39-related mechanisms in neurological diseases and is widely used in Alzheimer's disease research.

TM-N1324 (Standard) is the analytical standard of TM-N1324 (HY-108699). This product is intended for research and analytical applications. TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC₅₀s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.

TC-G-1008 (Standard) is the analytical standard of TC-G-1008 (HY-103007). This product is intended for research and analytical applications. TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC₅₀ values of 0.4 and 0.8 nM for rat and human receptors respectively.