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GPR

GPR119, a orphan receptor, couples to Gs so that GPR119 can upregulate the  intracellular cAMP obviously when GPR119 is expressed in high level.ATP-sensitive K+ and voltage-dependent Ca2+ channels are also involved in GPR119-mediated responses. GPR119 is involved in glucose-stimulated insulin secretion (GSIS), and GPR119 is also a beta-Cell-Specific GPCR and GPR119 is expressed highly in pancreatic islets and pancreatic β-cells so that researchers treat GPR119 as a potential target for drug development against type 2 diabetes.

Other GPCR & G Protein Related Inhibitors

Hedgehog/Smoothened PKA CGRP Receptor Endothelin Receptor S1P Receptor Cannabinoid Receptor SGLT Opioid Receptor CCR MT Receptor
Cat.No. Product Name Information Product Use Citations Product Validations
S8673 ONC212 ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. This compound is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.
Pharmacology Research & Perspectives, August 15, 2022, e00993
International Journal of Molecular Sciences, April 29, 2021, 4750
Mol Oncol, 2025, 10.1002/1878-0261.70081
S2637 Fasiglifam(TAK-875) Hemihydrate Fasiglifam(TAK-875) Hemihydrate is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.
Sci Rep, 2025, 15(1):11403
iScience, 2022, 104603
Endocrinology, 2021, 162(3)bqab002
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S8014 GW9508 GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, and stimulates insulin secretion in a glucose-sensitive manner.
J Enzyme Inhib Med Chem, 2021, 36(1):1651-1658
Bioorg Chem, 2020, 99:103830
Arch Pharm (Weinheim), 2020, e2000275
S5400 3-chloro-5-hydroxybenzoic Acid 3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81.
American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, November 01, 2022, R822-R831
Frontiers in Cell and Developmental Biology, January 14, 2026, 1699042
American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, January 07, 2026, Online ahead of print
S9477 AH7614 AH7614 (compound 39) is a selective FFA4 (GPR120) antagonist with pIC50s of 7.1 for human FFA4 and 8.1 for mouse FFA4.
Biochem Biophys Res Commun, 2025, 781:152546
Cell Prolif, 2023, e13551.
Cell Death Differ, 2021, 10.1038/s41418-021-00887-9
S6889 Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. This compound prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
Frontiers in Oncology, January 28, 2020, 22
Cell Cycle, December 8, 2022, 818-828
Cell Cycle, 2023, 818-828
S6759 TC-G-1008 (GPR39-C3) TC-G-1008 (GPR39-C3) is a potent and orally bioavailable agonist of GPR39 with EC50 of 0.4nM and 0.8nM for rat and human receptor, respectively.
Journal of Cachexia, Sarcopenia and Muscle, 2025, e13771
J Cachexia Sarcopenia Muscle, 2025, 16(2):e13771
Acta Biochimica et Biophysica Sinica, 2024, 2024218
S0135 JMS-17-2 JMS-17-2 is a potent and selective small-molecule antagonist of CX3C chemokine receptor 1 (CX3CR1/GPR13) with IC50 of 0.32 nM. This compound is used in the research of metastatic disease in breast cancer patients.
International Journal of Oncology, 2022, 47
Int J Oncol, 2022, 60(4)47
Brain Res Bull, 2021, S0361-9230(21)00289-6
S6850 NE 52-QQ57 NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. This compound effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with this chemical significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
Exp Hematol Oncol, 2024, 13(1):13
Current Issues in Molecular Biology, 2022, 1046-1061
S2149 GSK1292263 GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.
PLoS One, 2015, 10(7):e0134051
PLoS One, 2015, e0134051
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