GPR

NOX-6-18 (GPR132-B-160) is a highly potent and selective GPR132 antagonist with insulinotropic activity that modulates macrophage reprogramming in pancreatic islets and reduces weight gain.

BTB09089 (GPR65 agonist ) is a T cell death-associated gene 8 (TDAG8 GPR65)-specific agonist.BTB09089 induces TDAG8 expression and regulates cytokine production in T cells and macrophages.

GLPG0974 is an antagonist of FFA2 GPR43 with IC50 of 9 nM.

G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).

CAY10595 is an antagonist of the CRTh2 (DP2) receptor with a Ki of 10 nM.

GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK PD characteristics and can be used to study pulmonary fibrosis.

Prosaptide TX14(A) acetate is a potent GPR37L1 and GPR37 agonist. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells.

CVN424 is a selective and novel GPR6 Inverse agonist effective in models of Parkinson Disease.

Fasiglifam (TAK875) is a potent, selective and orally bioavailable GPR40 agonist.

ONC212 [a fluorinated-ONC201 analogue] is a selective GPR132 agonist.

VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.

LY2881835 is a potent and selective GPR40 agonist.

Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.

AM251 is a effective CB1 receptor antagonist (IC50 Ki: 8 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM).

CRTh2 antagonist 1 is a CRTh2 antagonist [IC50: 89 nM].

TAK-041 (NBI-1065846) is a potent and selective GPR139 agonist.

BIM-46174 HCl is a selective G protein inhibitor with anticancer activity that inhibits the growth of a large number of human cancer cell lines and induces cysteine 3-dependent apoptosis.

CID 2745687 is a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50 = 6.70. CID 2745687 cannot effectively antagonize the agonist effects of either Zaprinast or Cromolyn disodium at rodent ortholog of GPR35 in vitro[1]. However, CID 2745687 can reverse lodoxamide-mediated anti-fibrotic effects in mice in vivo[2].

Latanoprost (Xalatan) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.

HA15 targets specifically BiP GRP78 HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.

MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).

Bimatoprost acid (17-phenyl trinor PGF2α) is a metabolically stable analog of PGF2α and has a potential antagonistic activity for the FP receptor. It has a relative potency of 756% compared to PGF2α for binding to the FP receptor on ovine luteal cells.

LY2922470 reduces glucose levels along with significant enhancements in insulin and GLP-1, which is the potential for the treatment of type 2 diabetes mellitus (T2DM). LY2922470 is an effective, selective, and orally available agonist of the G protein-cou

Azenosertib (ZN-c3) is an orally active, specific GPR119 agonist. Azenosertib (ZN-c3) stimulates cell proliferation and improves pancreatic β-cell function. [1]

hGPR91 antagonist 3 is an orally active, potent, and selective hGPR91 antagonist. hGPR91 antagonist 3 is used to study hypertension, autoimmune diseases, and retinal angiogenesis. hGPR91 antagonist 3 has been shown to be effective in the treatment of hypertension, autoimmune disease, and retinal angiogenesis.

7-FluorotryptaMine HCl is a potent aromatic monoamine GPRC5A agonist that induces GPRC5A-mediated β-arrestin recruitment.7-FluorotryptaMine HCl can be used to study signalling pathways related to immunity and cancer.

Urotensin II (114-124), human acetate is an 11-amino acid residue peptide, is a potent vasoconstrictor and agonist for the orphan receptor GPR14.

AMG-009 is a selective and potent dual antagonist of CRTH2 and DP, with an IC50 value of 3 nM for CRTH2 and 12 nM for DP receptors.

Dehydroeffusol (Dehydro Effusol) possesses anti-cancer, anxiolytic and sedative properties. Dehydroeffusol inhibits gastric cancer cell growth and tumorigenicity by selectively inducing tumor-suppressive endoplasmic reticulum stress and a moderate apoptosis.

NF-56-EJ40 is an effective and highly selective antagonist of human SUCNR1 with an IC50 of 25 nM and a Ki of 33 nM.

ATC 0175 hydrochloride is an orally active melanocyte concentrating hormone 1 receptor antagonist that is potent and selective. ATC 0175 hydrochloride has affinity for MCH1R, MCH2R, MCH1, 5-HT2B receptors and 5-HT1A receptors with IC50s of 13.5 nM, >10,000 nM, 13 nM, 9.66 nM and 16.9 nM, respectively. ATC 0175 hydrochloride exhibits antidepressant and anxiolytic effects in animal models. aTC 0175 can be used to study depression and or anxiety disorders.

Questiomycin A is an antibiotic produced in crème fraiche with antibacterial and anticancer activities. Questiomycin A suppresses expression of GRP78, a cell-protective ER chaperone protein.

GW9508(GW 9508) is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.

Fezagepras sodium (Setogepram sodium salt) is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferative actions.

Grp94 Inhibitor-1 is a potent and selective inhibitor of Grp94 with an IC50 of 2 nM.

AH-7614 (AH 7614) is a selective and potent free fatty acid receptor 4 (FFA4 GPR120) antagonist.

Kynurenic acid (Quinurenic acid) is an endogenous tryptophan active metabolite, a triple antagonist of NMDA, glutamate, α7 nicotinic acetylcholine receptor, and an agonist of GPR35 CXCR8 with neuroprotective and anticonvulsant properties. It has neuroprotective and anticonvulsant properties and can be used to study neurodegeneration and metabolism-related diseases.

Kisspeptin-10, rat acetate is an endogenous ligand for the rodent kisspeptin receptor (KISS1, GPR54).

Ogremorphin (GPR68-IN-1) is a potent inhibitor of GPR68 with an EC50 of 170 nM, used in the study of autoimmune chronic inflammatory diseases [1].

3-Hydroxyoctanoic Acid is one of the hydroxy-carboxylic acids (HCAs) that serve as intermediates of energy metabolism. It is an agonist of the orphan receptor GPR109B.

PSB-CB5 (GPR18-IN-32)2 is a GRP18 antagonist with anti-inflammatory activity and can be used to study obesity and metabolic disorders.

Azathioprine (BW 57-322), an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.

AM-1638 is an orally active GPR40 FFA1 agonist, useful for studying type II diabetes.

Tetrahydromagnolol can activate cannabinoid (CB) receptors.

BMS-903452 is a potent and selective GPR119 agonist with an EC50 of 14 nM, indicated for the treatment of acute and chronic rodent diabetes. GPR119 is mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. BMS-903452 shows no significant inhibitory effect on 9 cytochrome P450 enzymes (IC50 > 40 μM), does not activate PXR (EC50 > 50 μM), and is not toxic to liver (HEPG2) cell lines.

Latanoprost acid is a selective agonist of prostanoid receptors and inhibits RANKL-induced osteoclastogenesis and function through the inhibition of c-fos NFATc1 pathway. Latanoprost acid can be used in studies about lowering pressure inside the eyes.

6-OAU (GTPL5846)(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

AF64394 is a selective inverse agonist of GPR3(pIC50 : 7.3)