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GPR Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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.
J Cachexia Sarcopenia Muscle, 2025, 16(2):e13771
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
S0208 6-OAU 6-OAU (GTPL5846, 6-n-octylaminouracil) is a surrogate agonist of G protein-coupled receptor 84 (GPR84) that activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with EC50 of 105 nM in the PI assay. This compound increases [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with EC50 of 512 nM.
J Orthop Surg Res, 2023, 18(1):3
E2660 Pamoic acid disodium Pamoic acid disodium, a potent GPR35 agonist with an EC50 value of 79 nM, induces GPR35a internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively, also potently recruits β-arrestin2 to GPR35 showing an antinociceptive effect.
Poult Sci, 2025, 104(2):104761
S0001 GSK137647A GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
S6976 TC-O 9311 TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM.
S6746 APD668 APD668 (JNJ28630368) is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
E1235 NF-56-EJ40 NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.
E7448 [Pyr1]-Apelin-13 [Pyr1]-Apelin-13 is one of the endogenous agonists of the APJ receptor with high binding affinity Kd of 4.5 nM for hAPJ, predominantly found in the myocardium and plasma. It exhibits analgesic effects and improves cardiovascular function, making it a promising candidate for neuropathic pain and heart failure research.
S0742 DC260126 DC260126, a small organic antagonist for GPR40 (FFAR1), dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50=6.28, 5.96, 7.07, 4.58 μM, respectively), reduces GTP-loading and ERK1/2 phosphorylation stimulated by linoleic acid in GPR40-CHO cells, suppresses palmitic acid potentiated glucose-stimulated insulin secretion, and negatively regulates GPR40 mRNA expression induced by oleic acid in Min6 cells.
E4875 Lodoxamide Lodoxamide (U-42585E free acid) is a potent agonist of GPR35 with an EC50 of 1 nM. It also inhibits eosinophil peroxidase release after IgA activation and reduces eosinophil cationic protein and eosinophil-derived neurotoxin, suggesting direct effects on eosinophils. It is a mast cell stabilizer used to treat asthma, allergic conjunctivitis, and superior limbic keratoconjunctivitis.
E2037 Kisspeptin-10 (human) Kisspeptin-10, human is a potent vasoconstrictor and inhibitor of angiogenesis, acts as a tumor metastasis suppressor via its receptor GPR54, inducing osteoblast differentiation via NFATc4-mediated BMP2 expression.
E1928New Azelaprag Azelaprag (AMG 986) is a potent agonist of apelin receptor (APJ) with an EC50 of 0.32 nM. It exhibits potential and can be used in Heart failure (HF) research.
E0347 AS1269574 AS 1269574, a small-molecule G protein-coupled receptor 119 (GPR119) agonist, has an EC50 of 2.5 μM in HEK293 cells transiently expressing human GPR119 and enhances insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8 mM) conditions.
E4773New NOX-6-18（GPR132-B-160） NOX-6-18 (GPR132-B-160) is a potent and selective antagonist of GPR132 with an IC50 of 17 nM. It regulates macrophage reprogramming within pancreatic islets, reduces weight gain, and improves glucose metabolism in mice on a high-fat diet.
S0083 DJ-V-159 DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
E7663 O-1602 O-1602 is a potent agonist of G-protein coupled receptor 55 (GPR55). It exhibits anxiolytic and antidepressant effects by preventing Methamphetamine (METH)-induced hippocampal neurogenic damage and neuroinflammation, as well as stress from chronic social defeat.
S0110 APD597 APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
E0113 GPR84 antagonist 8 GPR84 antagonist 8 is an antagonist of GPR84,which abrogates the enhanced inflammatory response mediated by 6-OAU. It has the potential to reduce the inflammatory responses associated with the activation of the GPR84 receptor.
E7690 7α,25-Dihydroxycholesterol 7α,25-Dihydroxycholesterol (7α,25-OHC) is a potent and selective endogenous agonist of the orphan G protein-coupled receptor EBI2 (GPR183). It exhibits high potency in activating EBI2, with an EC50 of 140 pM and a Kd of 450 pM.
S6425 JNJ 63533054 JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.
E0106 ML401 ML401, a potent chemical probe, selectively antagonizes G-protein coupled receptor 183 (GPR183, EBI2) with an IC50 of 1.03 nM, and displays activity in a chemotaxis assay with IC50 of 6.24 nM.
S0156 CID 1375606 CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.
S2822 OC000459 OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2.
S0183 NIBR189 NIBR189 is a potent antagonist of the Epstein-Barr virus-induced gene 2 (EBI2, GPR183) receptor with IC50 of 16 nM for binding and 11 nM for function, respectively.
S2954 4-CMTB 4-CMTB is a selective allosteric agonist of free fatty acid receptor 2(FFA2, GPR43) with pEC50 of 6.38.
E1922 OX04528 OX04528 (compound 68) is a potent and G-protein-biased agonist of G protein-coupled receptor 84 (GPR84). This compound inhibits cAMP production with an EC50 value of 0.00598 nM (5.98 pM), respectively.
S3451 PH-064 PH-064 (BIM-46187) is a novel imidazo-pyrazine derivative that inhibits the heterotrimeric G-protein complex effectively. This compound inhibits heterotrimeric G-protein signalling in GPCRsthat mediate cyclic AMP generation (GAs), calcium release (GAq), cancer cell invasion by Wnt-2 frizzled receptors, and high-affinity neurotensin receptors (GAo/i and GAq).
S6651 G15 G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.
Biol Pharm Bull, 2025, 48(5):657-671
iScience, 2024, 27(3):109125
Nutrients, 2023, 16(1)38
S0851 G-1 (LNS 8801) G-1 (LNS 8801) is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.
iScience, 2024, 27(3):109125
E1768 MEDICA16 MEDICA16 is an inhibitor of ATP-citrate lyase and also acts as an agonist of G protein-coupled receptor 40 (GPR40). It functions to blunt the development of insulin resistance in the JCR:LA-cp rat as well as it is a potent triacylglycerol-lowering agent.
E7046 TRAP-6 TRAP-6 (PAR-1 agonist peptide) is a synthetic hexapeptide (SFLLRN) that acts as a agonist of PAR-1 (protease-activated receptor-1). It also activates GPR15 on T-cells, regulating immune responses by suppressing acute GvHD while maintaining GvT activity.
E0377 CLP-3094 CLP-3094, a potent inhibitor targeting the binding function 3 (BF3) site of androgen receptor (AR), inhibits AR transcriptional activity with IC50 of 4 μM, also is a selective, potent GPR142 antagonist.
S4709 Latanoprost Latanoprost (Xalatan, PhXA41) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. This compound increases uveoscleral outflow and thereby reduces intraocular pressure.
S4440 2-Phenylacetamide 2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells.