GPR

AR 231453 is a selective and orally available GPR119 agonist,can stimulate β-cell replication and improve islet graft function.

Ginsenoside Rb2 (Ginsenoside C) found in species of Panax, upregulating GPR120 gene expression.

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.

PU-WS13 hydrobromide is a GRP94 inhibitor with anti-inflammatory activity and inhibits the proliferation of M2-like macrophages in mouse TNBC tumors.

1-methoxycyclopropanecarboxylic acid is an agonist of free fatty acid receptor 3 (FFAR3, human).

FL104 is a potent agonist of small-molecule urotensin II receptor, pEC50= 7.11.

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

Urotensin II, mouse acetate (9047-55-6 free base) is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.

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

[Orn8]-Urotensin II acetate is a Urotensin receptor ligand and a partial agonist at Urotensin receptors.

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

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

2-(pentylsulfanyl)pyrimidine-4,6-diol is a novel GRP84 agonist.

(2-{[2-(2-fluorophenoxy)ethyl]sulfanyl}-1H-benzimidazol-1-yl)acetic acid is a prostaglandin-like CRTH2 antagonist with an IC50 < 10 μM, which can be used in studies of rhinitis, COPD, rheumatoid arthritis, eczema and conjunctivitis.

CRTh2 antagonist 1 is a CRTh2 antagonist (IC50: 89 nM).

Kisspeptin-10, human TFA is a potent vasoconstrictor and angiogenesis inhibitor. Kisspeptin-10, human TFA acts as a tumor metastasis suppressor via its receptor GPR54. Kisspeptin-10-GPR54 system plays an important role in embryonic kidney development. Kisspeptin-10/GPR54 signaling induces osteoblast differentiation via NFATc4-mediated BMP2 expression

Kisspeptin 234 acetate(1145998-81-7 free base) is a Kisspeptin receptor (KISS1, GPR54) antagonist; a Kisspeptin-10 analogue. It inhibits the stimulation of inositol phosphate (IP) (IC50 = 7 nM) and the release of gonadotropin-releasing hormone (GnRH) by kisspeptin-10.

BigLEN (mouse) acetate is a potent and selective agonist of orphan G protein-coupled receptor 171 (GPR171), with a Kd of ∼0.5 nM.

(1S,2R)-2-PCCA is a novel and potent small molecule GPR88 receptor agonist with an EC50 value of 3 nM in the non-cellular system and 603 nM in the cellular system.

LY2881835 is a specific G protein-coupled receptor 40 (GPR40) agonist with potential hypoglycemic activity that enhances glucose-stimulated insulin secretion in normal lean mice.LY2881835 has been used in the study of type 2 diabetes.

MCH(human, mouse, rat) is a potent endogenous agonist at melanin-concentration hormone (MCH) receptors (IC50 values are 0.3 and 1.5 nM and EC50 values are 3.9 and 0.1 nM at MCH1 and MCH2 receptors respectively). Increases food intake in vivo.

[Orn5]-URP acetate is an effective and selective Urotensin-II receptor (UT) antagonist (pEC50 = 7.24). [Orn5]-URP exhibits no agonist activity.

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

CRTh2 antagonist 2 is a selective and potent CRTH2 antagonist, IC50≤10 nM. CRTh2 antagonist 2 can be used to study the direction of androgenic alopecia.

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

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.

GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively.

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.

YE 120 is a highly potent GPR35 agonist (EC50: 32.5 nM) with potential anti-inflammatory and anti-cancer activities, which can be used to study G protein-coupled receptor-related diseases.

GPR84 antagonist 8 is a selective GPR84 antagonist.

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

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.

TUG-1375 is an Agonist of Thiazolidine Free Fatty Acid Receptor 2

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).

GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis.

TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) agonist (EC50: 7.39).TUG-499 has an affinity for FFAR1 or GPR40 over the related receptors FFA2, FFA3 and the nuclear receptor PPARγ, as well as other different receptors, ion channels and transporter proteins.TUG-499 can be used to study type 2 Type 2 diabetes.

NE 52-QQ57 is a selective, and orally available antagonist of GPR4(IC50 : 70 nM),with anti-inflammatory activity.

GPR120 Agonist 2 is a potent and selective GPR120 receptor agonist.

2-Oleoylglycerol is a lipid found in palm kernel, sunflower seed and rice bran.2-Oleoylglycerol acts as a GPR119 agonist with neuroprotective effects and induces secretion of glucagon-like peptide 1 (GLP-1).2-Oleoylglycerol is used in the modelling of non-alcoholic steatohepatitis.

15(R)-15-methyl Prostaglandin D2 (15(R)15methyl PGD2) is a synthetic analogue of PGD2 and a selective and potent CRTH2/DP2 receptor agonist that modulates eosinophil CD11b expression, actin polymerisation and chemotaxis.

PSN 375963 (PSN 375963 hydrochloride) hydrochloride is a synthetic agonist of the endogenous ligand for GPR119.

Benzyl nicotinate (Pycaril) is a agonist of GPR109A receptor and GPR109B receptor

Myristyl nicotinate (Tetradecyl nicotinate) is an ester prodrug being developed for delivery of nicotinic acid (NIC) into the skin for prevention of actinic keratosis and its progression to skin cancer.

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.

Palosuran hydrochloride 540769-28-6(free base)(ACT-058362 hydrochloride) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.

GPCR agonist-2 (4-(Cyclopropylamino)-3-nitrobenzoic acid) is an agonist of the orphan human GPCR GPR109B.

(+/-)-Pinocembrin (NSC-43318), a natural product from axillary pines, is a GPR120 ligand that promotes wound healing in the HaCaT cell line.

TC-O 9311 is a potent GPR139 agonist.

Acifran (AY 25712) is an HM74A/GPR109A and GPR109B agonist and displays antihyperlipidemic activity.

Ogremorphin (OGM) is a selective and potent GPR68 inhibitor (EC50: 170 nM), which can be used to study autoimmune chronic inflammatory diseases.