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GPR

G-protein coupled receptors (GPRs) are a family of seven-transmembrane receptors, which play an important role in the response to peptide hormones, neurotransmitters, and free fatty acids.

CVN424
T93462254706-21-1
CVN424 is a selective and novel GPR6 Inverse agonist effective in models of Parkinson Disease.
  • $97
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NOX-6-18
T83972898211-21-7
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.
  • $68
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BTB09089
T67892245728-44-3In house
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.
  • $65
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VER-155008
T70101134156-31-2
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.
  • $39
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AM251
T1915183232-66-8
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).
  • $43
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Fasiglifam
T23511000413-72-8
Fasiglifam (TAK875) is a potent, selective and orally bioavailable GPR40 agonist.
  • $45
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FTBMT
T153521358575-02-6
FTBMT is a selective GPR52 agonist (EC50: 75 nM) and has antipsychotic and procognitive properties.
  • $44
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Dihydromunduletone
T11044674786-20-0
Dihydromunduletone (DHM) is an adhesion G protein-coupled receptor (aGPCR) antagonist that acts as a chemical probe for the inhibition of GPR56 and GPR114 ADGRG5, which have similar tethered agonists.
  • $179
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Prosaptide TX14(A) acetate
TP1970L
Prosaptide TX14(A) acetate is a potent GPR37L1 and GPR37 agonist. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells.
  • $148
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YE 120
T23542383124-82-1In house
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.
  • $97
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LY2881835
T279371292290-38-0In house
LY2881835 is a potent and selective GPR40 agonist.
  • $293
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BIM-46174 HCl
T70039L In house
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.
  • $133
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G-1
T15364881639-98-1
G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).
  • $43
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NF-56-EJ40
T122162380230-73-7
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.
  • $83
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cangrelor tetrasodium
T5036163706-36-3
Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.
  • $39
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Latanoprost
T2528130209-82-4
Latanoprost (Xalatan) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.
  • $39
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Fezagepras
T128831002101-19-0
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.
  • $48
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HA15
T68551609402-14-3
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.
  • $34
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GPR81 agonist 1
T626561620992-67-7
GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.
  • $132
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GPR35 agonist 2
T23434494191-73-0In house
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.
  • $44
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Bimatoprost acid
T2093938344-08-0
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.
  • $135
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GLPG1205
T114111445847-37-9In house
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.
  • $88
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CID 2745687
T21874264233-05-8
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].
  • $34
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AR 231453
T8329733750-99-7
Azenosertib (ZN-c3) is an orally active, specific GPR119 agonist. Azenosertib (ZN-c3) stimulates cell proliferation and improves pancreatic β-cell function. [1]
  • $30
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hGPR91 antagonist 3
T628581314796-31-0
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.
  • $149
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GLPG0974
T153881391076-61-1
GLPG0974 is an antagonist of FFA2/GPR43 with IC50 of 9 nM.
  • $51
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TAK-041
T93171929519-13-0
TAK-041 (NBI-1065846) is a potent and selective GPR139 agonist.
  • $31
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7-FluorotryptaMine HCl
T77673159730-09-3
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.
  • $31
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Urotensin II (114-124), human acetate
TP1737L
Urotensin II (114-124), human acetate is an 11-amino acid residue peptide, is a potent vasoconstrictor and agonist for the orphan receptor GPR14.
  • $196
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CRTh2 antagonist 1
T100841379445-54-1In house
CRTh2 antagonist 1 is a CRTh2 antagonist [IC50: 89 nM].
  • $117
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AMG-009
T142111027847-67-1
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.
  • $41
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Fezagepras sodium
T123751254472-97-3In house
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.
  • $36
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MS21570
T582865373-29-7
MS21570 as a GPR171 antagonist based on its ability to block,with an IC50 of 220 Nm,that reduces anxiety-like behavior and fear conditioning in mice.
  • $38
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CAY10471 Racemate
T7359844639-57-2
CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective CRTH2 DP2 receptor antagonist. It binds to human CRTH2 DP2, DP1, and TP receptors with Ki values of 0.6, 1200, and >10,000 nM, respectively.
  • $43
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Questiomycin A
T368181916-59-2
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.
  • $50
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Kisspeptin 234 acetate(1145998-81-7 free base)
TP1896L1
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.
  • $148
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AH-7614
T220276326-06-3
AH-7614 (AH 7614) is a selective and potent free fatty acid receptor 4 (FFA4 GPR120) antagonist.
  • $47
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LY2922470
T158101423018-12-5
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
  • $117
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Grp94 Inhibitor-1
T72612234897-35-7
Grp94 Inhibitor-1 is a potent and selective inhibitor of Grp94 with an IC50 of 2 nM.
  • $41
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4-CMTB
T8642300851-67-6
4-CMTB is a selective agonist of FFA2 and GPR43.It also is a positive allosteric modulator (pEC50=6.38).
  • $41
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AF64394
T84071637300-25-4
AF64394 is a selective inverse agonist of GPR3(pIC50 : 7.3)
  • $33
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FL104
T27328885672-81-1In house
FL104 is a potent agonist of small-molecule urotensin II receptor, pEC50= 7.11.
  • $118
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2-Oleoylglycerol
T375263443-84-3
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.
  • $95
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CAY10595
T10691916047-16-0In house
CAY10595 is an antagonist of the CRTh2 (DP2) receptor with a Ki of 10 nM.
  • $46
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PSB-CB5
T270191627710-30-8
PSB-CB5 (GPR18-IN-32)2 is a GRP18 antagonist with anti-inflammatory activity and can be used to study obesity and metabolic disorders.
  • $81
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APD668
T2088832714-46-2
APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.
  • $45
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Latanoprost acid
T1571841639-83-2
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.
  • $52
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GSK137647A
T3171349085-82-1
GSK137647A (GSK 137647) is a selective agonist of FFA4.
  • $30
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