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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
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
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
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
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
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
Verified customer review of GSK1292263
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.
E6710New MKP10241 MKP10241 is a potent, orally active agonist of GPR119 that elevates cAMP levels in a GPR119‑expressing cell line with an EC50 ≈ 3.7 nM. MKP10241 reduces blood glucose and HbA1c in acute and chronic diabetic mouse models and shows excellent preclinical efficacy in rodent models of obesity and MASH.
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.
E6776New AP-503 AP‑503 is a selective agonist of GPR133/ADGRD1 with an EC50 of 1.21 nM. It exhibits the potential to be used in research on the prevention of muscle‑related diseases and vestibular dysfunction.
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.