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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.

  • AR 231453
    T8329733750-99-7
    AR 231453 is a selective and orally available GPR119 agonist,can stimulate β-cell replication and improve islet graft function.
    • $30
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  • Ginsenoside Rb2
    T391911021-13-9
    Ginsenoside Rb2 (Ginsenoside C) found in species of Panax, upregulating GPR120 gene expression.
    • $90
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  • Kynurenic acid
    T65135492-27-3
    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.
    • $31
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  • Urotensin II, mouse acetate (9047-55-6 free base)
    TP2165
    Urotensin II, mouse acetate (9047-55-6 free base) is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.
    • $168
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  • FL104
    T27328885672-81-1In house
    FL104 is a potent agonist of small-molecule urotensin II receptor, pEC50= 7.11.
    • $197
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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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  • PU-WS13 hydrobromide
    T5351L
    PU-WS13 hydrobromide is a GRP94 inhibitor with anti-inflammatory activity and inhibits the proliferation of M2-like macrophages in mouse TNBC tumors.
    • $36
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  • 1-methoxycyclopropanecarboxylic acid
    T9437100683-08-7
    1-methoxycyclopropanecarboxylic acid is an agonist of free fatty acid receptor 3 (FFAR3, human).
    • $50
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  • [Orn8]-Urotensin II acetate
    T37527L
    [Orn8]-Urotensin II acetate is a Urotensin receptor ligand and a partial agonist at Urotensin receptors.
    • $195
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  • Kisspeptin-10, rat acetate(478507-53-8 free base)
    TP1666L
    Kisspeptin-10, rat acetate is an endogenous ligand for the rodent kisspeptin receptor (KISS1, GPR54).
    • $93
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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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  • BMS-903452
    T677911339944-47-6In house
    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.
    • $154
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  • 2-(pentylsulfanyl)pyrimidine-4,6-diol
    T50078489403-70-5
    2-(pentylsulfanyl)pyrimidine-4,6-diol is a novel GRP84 agonist.
    • $126
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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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  • WAY-298630
    T77601303134-93-2
    (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.
    • $195
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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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  • Kisspeptin-10, human (TFA)(374675-21-5,FREE)
    TP1345
    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
    • $115
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  • BigLEN (mouse) acetate
    TP2073L
    BigLEN (mouse) acetate is a potent and selective agonist of orphan G protein-coupled receptor 171 (GPR171), with a Kd of ∼0.5 nM.
    • $148
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  • (1S,2R)-2-PCCA
    T13423L In house
    (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.
    • $195
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  • LY2881835
    T279371292290-38-0
    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.
    • $293
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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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  • [Orn5]-URP acetate
    TP1928L1
    [Orn5]-URP acetate is an effective and selective Urotensin-II receptor (UT) antagonist (pEC50 = 7.24). [Orn5]-URP exhibits no agonist activity.
    • $297
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  • MCH(human, mouse, rat)
    TP1996128315-56-0
    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.
    • $228
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  • CRTh2 antagonist 2
    T10889780763-95-3In house
    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.
    • $109
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  • MEDICA16
    T2296787272-20-6In house
    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.
    • $58
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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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  • 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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  • 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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  • 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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  • 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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  • GPR84 antagonist 8
    T114621445846-30-9In house
    GPR84 antagonist 8 is a selective GPR84 antagonist.
    • $1,670
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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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  • GPR35 agonist 3
    T72755123021-85-2
    GPR35 agonist 3 is a synthetic GPR35 agonist with an EC50 value of 1.4 μg in the β-arrestin recruitment assay.GPR35 agonist 3 is used in the study of cancer, type 2 diabetes, and cardiovascular disease.
    • $42 TargetMol
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  • ONC212
    T73981807861-48-8
    ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132.
    • $44
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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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  • Grp94 Inhibitor-1
    T72612234897-35-7
    Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor (IC50 : 2 nM).
    • $41
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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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  • TUG-1375
    T77962247372-59-2
    TUG-1375 is an Agonist of Thiazolidine Free Fatty Acid Receptor 2
    • $135
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  • MK-6892
    TQ0108917910-45-3
    MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).
    • $115
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  • Azathioprine
    T1237446-86-6
    Azathioprine (BW 57-322), an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.
    • $45
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  • GSK137647A
    T3171349085-82-1
    GSK137647A (GSK 137647) is a selective FFA4 agonist.
    • $30
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  • GW9508
    T1781885101-89-3
    GW9508(GW 9508) is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.
    • $45
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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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  • 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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  • 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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  • 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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  • GSK256073
    T15432862892-90-8
    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.
    • $67
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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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  • GPR120 Agonist 2
    T43121234844-11-1
    GPR120 Agonist 2 is a potent and selective GPR120 receptor agonist.
    • $54
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  • TUG-499
    T601841206629-08-4
    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.
    • $48
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