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GPR Agonists

Cat.No. Product Name Information Product Use Citations Product Validations
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
Endocrinology, 2021, 162(3)bqab002
Psychopharmacology (Berl), 2021, 10.1007/s00213-021-05837-4
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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
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.
Mol Oncol, 2025, 10.1002/1878-0261.70081
Oncogenesis, 2025, 14(1):20
Elife, 2024, 12RP91313
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, 2026, Online ahead of print
MedComm (2020), 2023, 4(2):e242
MedComm, 2023, e242
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.
Cell Cycle, 2023, 818-828
Cell Cycle, 2022, 1-11.
Aging (Albany NY), 2021, 17097-17117
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
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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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
Journal of Orthopaedic Surgery and Research, 2023, 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
Poultry Science, 2025, 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.
E6509New AR420626 AR420626 is a selective agonist of FFAR3 (GPR41) with an IC50 of 117 nM, that prevents serotonin-induced circular muscle relaxation ex vivo and defecation in vivo.
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.
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.
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).
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.
S0156 CID 1375606 CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.
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.
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.
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.