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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.
Cat No. product name
TP1928L1 [Orn5]-URP acetate [Orn5]-URP acetate 是一种有效的选择性 Urotensin-II receptor (UT) 拮抗剂 (pEC50 = 7.24)。 [Orn5]-URP 没有激动剂活性。
T37527L [Orn8]-Urotensin II acetate [Orn8]-Urotensin II acetate 是一种 Urotensin 受体配体和 Urotensin 受体的部分激动剂。
TN1560 Dehydroeffusol Dehydroeffusol possesses anti-cancer, anxiolytic and sedative properties, it may antagonize the spasmogenic activity of various agents, and therefore, could be a...
T7359 CAY10471 Racemate CAY 10471 is a potent, highly selective CRTH2/DP 2 receptor antagonist. CAY10471 binds to the human CRTH2/DP2, DP1, and TP receptors( Ki values of 0.6, 1200, and...
T3919 Ginsenoside Rb2 Ginsenoside Rb2 found in species of Panax, upregulating GPR120 gene expression.
T5406 SNAP 94847 SNAP-94847 is a selective and competitive MCH1 receptor (MCH1-R) antagonist (Ki: 2.2 nM). It has anxiolytic and antidepressant activity and reduces food intake i...
TP1996 MCH(human, mouse, rat) 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 re...
T36818 Questiomycin A Questiomycin A is an antibiotic produced in crème fraiche with antibacterial and anticancer activities. Questiomycin A suppresses expression of GRP78, a cell-pro...
T15364 G-1 G-1 is a nonsteroidal, high-affinity and selective GPR30 agonist (Ki: 11 nM).
T7261 Grp94 Inhibitor-1 Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor (IC50 : 2 nM).
T7010 VER-155008 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 se...
T2396 Ramatroban Ramatroban (BAY u3405) is a thromboxane A(2) (TxA(2)) antagonist marketed for allergic rhinitis. It has been used in trials studying the treatment of Asthma.
T23204 PSN 375963 GPR119 receptor agonist
T8004 SNAP 94847 hydrochloride SNAP 94847 hydrochloride is a melanin-concentrating hormonereceptor1 (MCHR1) antagonist(Ki= 2.2 nM)
T12095 Monomethyl fumarate Monomethyl fumarate is a potent agonist of GPR109A .
TP2073L BigLEN (mouse) acetate BigLEN (mouse) acetate is a potent and selective agonist of orphan G protein-coupled receptor 171 (GPR171), with a Kd of ∼0.5 nM.
T2528 Latanoprost Latanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.
T2088 APD668 APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.
T6399 AZD1981 AZD1981 is an effective and specific CRTh2 (DP2) receptor antagonist (IC50: 4 nM), showing >1000-fold selectivity over more than 340 other enzymes and receptors,...
T9317 TAK-041 TAK-041 is a potent and selective GPR139 agonist.
T5100 DJ-V-159 DJ-V159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
T1237 Azathioprine Azathioprine, an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.
T19700 IBC 293 IBC 293 is selective for GPR109B over niacin receptor GPR109A. IBC 293 is a highly selective agonist for GPR109B, a human orphan G-protein-coupled receptor expre...
T1781 GW9508 GW9508 is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.
T8901 YUM70 YUM70 is a potent and selective glucose-regulated protein 78 (GRP78) inhibitor(with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length pro...
T5036 Cangrelor tetrasodium Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.
T15810 LY2922470 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 (...
T7127 DC260126 DC260126 is a small-molecule antagonist of FFA1 (GPR40)
T3965 Fevipiprant Fevipiprant is a selective, potent, reversible competitive CRTh2 antagonist.
T19438 Myristyl nicotinate Myristyl nicotinate is an ester prodrug and a lipophilic derivative of Nicotinic acid.
TN1849 Kuwanon H Kuwanon H, and possibly kuwanon G also, are specific antagonists for the gastrin-releasing peptide (GRP) -preferring receptor and can be useful for studying the ...
TP1970L Prosaptide TX14(A) acetate Prosaptide TX14(A) acetate is a potent GPR37L1 and GPR37 agonist. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells.
T7398 ONC212 ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132.
T6855 HA15 HA15 targets specifically BiP/GRP78/HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells t...
T2664 Timapiprant OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist (IC50: 13 nM).
T3520 Setipiprant Setipiprant is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced b...
T9719 3-Hydroxyoctanoic Acid 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 GP...
T15432 GSK256073 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...
T14565 BI-671800 BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2). With IC50 values of 4.5 nM and 3.7...
T1286 Vincamine Vincamine is a major alkaloid of Vinca minor L., Apocynaceae. It has been used therapeutically as a vasodilator and antihypertensive agent, particularly in cereb...
T50078 2-(pentylsulfanyl)pyrimidine-4,6-diol 2-(pentylsulfanyl)pyrimidine-4,6-diol is a novel GRP84 agonist.
T1915 AM251 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 ...
T2036 6-OAU 6-OAU(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 ...
T20939 Bimatoprost acid Bimatoprost acid is a metabolically stable analog of PGF2α and has a potential antagonistic activity for the FP receptor. It has a relative potency of 756% compa...
T2058 Palosuran Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor.
T21623 AS1269574 AS 1269574 is a potent, orally available GPR119 agonist. AS1269574 has the potential for the research of type 2 diabetes.
T1793 MBX-2982 MBX-2982 is a selective, orally-available GPR119 agonist, used for the treatment of diabetes.
T22027 AH-7614 AH 7614 is a selective and potent free fatty acid receptor 4 (FFA4/GPR120) antagonist.
T21874 CID 2745687 CID 2745687 is a GPR35 antagonist that inhibited the effects at human GPR35 of cromolyn disodium and zaprinast, two agonists that share an overlapping binding s...
T2351 Fasiglifam TAK875 is a potent, selective and orally bioavailable GPR40 agonist.
[Orn5]-URP acetate
TP1928L1
[Orn5]-URP acetate 是一种有效的选择性 Urotensin-II receptor (UT) 拮抗剂 (pEC50 = 7.24)。 [Orn5]-URP 没有激动剂活性。
[Orn8]-Urotensin II acetate
T37527L
[Orn8]-Urotensin II acetate 是一种 Urotensin 受体配体和 Urotensin 受体的部分激动剂。
Dehydroeffusol
TN1560
Dehydroeffusol possesses anti-cancer, anxiolytic and sedative properties, it may antagonize the spasmogenic activity of various agents, and therefore, could be a...
CAY10471 Racemate
T7359
CAY 10471 is a potent, highly selective CRTH2/DP 2 receptor antagonist. CAY10471 binds to the human CRTH2/DP2, DP1, and TP receptors( Ki values of 0.6, 1200, and...
Ginsenoside Rb2
T3919
Ginsenoside Rb2 found in species of Panax, upregulating GPR120 gene expression.
SNAP 94847
T5406
SNAP-94847 is a selective and competitive MCH1 receptor (MCH1-R) antagonist (Ki: 2.2 nM). It has anxiolytic and antidepressant activity and reduces food intake i...
MCH(human, mouse, rat)
TP1996
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 re...
Questiomycin A
T36818
Questiomycin A is an antibiotic produced in crème fraiche with antibacterial and anticancer activities. Questiomycin A suppresses expression of GRP78, a cell-pr...
G-1
T15364
G-1 is a nonsteroidal, high-affinity and selective GPR30 agonist (Ki: 11 nM).
Grp94 Inhibitor-1
T7261
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor (IC50 : 2 nM).
VER-155008
T7010
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...
Ramatroban
T2396
Ramatroban (BAY u3405) is a thromboxane A(2) (TxA(2)) antagonist marketed for allergic rhinitis. It has been used in trials studying the treatment of Asthma.
PSN 375963
T23204
GPR119 receptor agonist
SNAP 94847 hydrochloride
T8004
SNAP 94847 hydrochloride is a melanin-concentrating hormonereceptor1 (MCHR1) antagonist(Ki= 2.2 nM)
Monomethyl fumarate
T12095
Monomethyl fumarate is a potent agonist of GPR109A .
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.
Latanoprost
T2528
Latanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.
APD668
T2088
APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.
AZD1981
T6399
AZD1981 is an effective and specific CRTh2 (DP2) receptor antagonist (IC50: 4 nM), showing >1000-fold selectivity over more than 340 other enzymes and receptors,...
TAK-041
T9317
TAK-041 is a potent and selective GPR139 agonist.
DJ-V-159
T5100
DJ-V159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
Azathioprine
T1237
Azathioprine, an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.
IBC 293
T19700
IBC 293 is selective for GPR109B over niacin receptor GPR109A. IBC 293 is a highly selective agonist for GPR109B, a human orphan G-protein-coupled receptor expre...
GW9508
T1781
GW9508 is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.
YUM70
T8901
YUM70 is a potent and selective glucose-regulated protein 78 (GRP78) inhibitor(with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length pr...
cangrelor tetrasodium
T5036
Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.
LY2922470
T15810
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 (...
DC260126
T7127
DC260126 is a small-molecule antagonist of FFA1 (GPR40)
Fevipiprant
T3965
Fevipiprant is a selective, potent, reversible competitive CRTh2 antagonist.
Myristyl nicotinate
T19438
Myristyl nicotinate is an ester prodrug and a lipophilic derivative of Nicotinic acid.
Kuwanon H
TN1849
Kuwanon H, and possibly kuwanon G also, are specific antagonists for the gastrin-releasing peptide (GRP) -preferring receptor and can be useful for studying the ...
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.
ONC212
T7398
ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132.
HA15
T6855
HA15 targets specifically BiP/GRP78/HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells t...
Timapiprant
T2664
OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist (IC50: 13 nM).
Setipiprant
T3520
Setipiprant is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced b...
3-Hydroxyoctanoic Acid
T9719
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 GP...
GSK256073
T15432
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...
BI-671800
T14565
BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2). With IC50 values of 4.5 nM and 3.7...
Vincamine
T1286
Vincamine is a major alkaloid of Vinca minor L., Apocynaceae. It has been used therapeutically as a vasodilator and antihypertensive agent, particularly in cereb...
2-(pentylsulfanyl)pyrimidine-4,6-diol
T50078
2-(pentylsulfanyl)pyrimidine-4,6-diol is a novel GRP84 agonist.
AM251
T1915
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 ...
6-OAU
T2036
6-OAU(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 ...
Bimatoprost acid
T20939
Bimatoprost acid is a metabolically stable analog of PGF2α and has a potential antagonistic activity for the FP receptor. It has a relative potency of 756% comp...
Palosuran
T2058
Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor.
AS1269574
T21623
AS 1269574 is a potent, orally available GPR119 agonist. AS1269574 has the potential for the research of type 2 diabetes.
MBX-2982
T1793
MBX-2982 is a selective, orally-available GPR119 agonist, used for the treatment of diabetes.
AH-7614
T22027
AH 7614 is a selective and potent free fatty acid receptor 4 (FFA4/GPR120) antagonist.
CID 2745687
T21874
CID 2745687 is a GPR35 antagonist that inhibited the effects at human GPR35 of cromolyn disodium and zaprinast, two agonists that share an overlapping binding s...
Fasiglifam
T2351
TAK875 is a potent, selective and orally bioavailable GPR40 agonist.
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