GPR

GPR製品

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  • GPR阻害剤 (1)
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  • GPR拮抗剤(13)
  • GPR作動薬(19)
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S2637 Fasiglifam(TAK-875) Hemihydrate Fasiglifam(TAK-875) Hemihydrate is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.
Endocrinology, 2021, 162(3)bqab002
Psychopharmacology (Berl), 2021, 10.1007/s00213-021-05837-4
Environ Sci Technol, 2020, 54(6):3428-3436
S8014 GW9508 GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner.
J Enzyme Inhib Med Chem, 2021, 36(1):1651-1658
Bioorg Chem, 2020, 99:103830
Arch Pharm (Weinheim), 2020, e2000275
S6651 G15 G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.
iScience, 2024, 27(3):109125
Nutrients, 2023, 16(1)38
Chem Biol Interact, 2023, 10.1016/j.cbi.2023.110728
S8673 ONC212 ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.
OPARU, 2023, 10.18725/OPARU-48122
Pharmacol Res Perspect, 2022, 10(4):e00993
Front Pharmacol, 2021, 12:737637
S9477 AH7614 AH7614 (compound 39) is a selective FFA4 (GPR120) antagonist with pIC50s of 7.1 for human FFA4 and 8.1 for mouse FFA4.
Cell Prolif, 2023, e13551.
Cell Death Differ, 2021, 10.1038/s41418-021-00887-9
S0135 JMS-17-2 JMS-17-2 is a potent and selective small-molecule antagonist of CX3C chemokine receptor 1 (CX3CR1/GPR13) with IC50 of 0.32 nM. JMS-17-2 is used in the research of metastatic disease in breast cancer patients.
Int J Oncol, 2022, 60(4)47
Brain Res Bull, 2021, S0361-9230(21)00289-6
S6889 Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
Cell Cycle, 2022, 1-11.
Aging (Albany NY), 2021, 13(13):17097-17117
S2149 GSK1292263 GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.
PLoS One, 2015, 10(7):e0134051
S7263 AZD1981 AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2.
Mol Cancer Ther, 2019, 18(11):2097-2110
S5400 3-chloro-5-hydroxybenzoic Acid 3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81.
MedComm (2020), 2023, 4(2):e242
MedComm (2020), 2023, 4(2):e242
Antioxidants (Basel), 2023, 12(12)2087
S0208 6-OAU 6-OAU (GTPL5846, 6-n-octylaminouracil) is a surrogate agonist of G protein-coupled receptor 84 (GPR84) that activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with EC50 of 105 nM in the PI assay. 6-OAU (GTPL5846, 6-n-octylaminouracil) increases [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with EC50 of 512 nM.
J Orthop Surg Res, 2023, 18(1):3
S0001 GSK137647A GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
S6976 TC-O 9311 TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM.
S6746 APD668 APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
E1235 NF-56-EJ40 NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.
S0742 DC260126 DC260126, a small organic antagonist for GPR40 (FFAR1), dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50=6.28, 5.96, 7.07, 4.58 μM, respectively), reduces GTP-loading and ERK1/2 phosphorylation stimulated by linoleic acid in GPR40-CHO cells, suppresses palmitic acid potentiated glucose-stimulated insulin secretion, and negatively regulates GPR40 mRNA expression induced by oleic acid in Min6 cells.
E2037 Kisspeptin-10 (human) Kisspeptin-10, human is a potent vasoconstrictor and inhibitor of angiogenesis, acts as a tumor metastasis suppressor via its receptor GPR54, inducing osteoblast differentiation via NFATc4-mediated BMP2 expression.
E0347 AS1269574 AS 1269574, a small-molecule G protein-coupled receptor 119 (GPR119) agonist, has an EC50 of 2.5 μM in HEK293 cells transiently expressing human GPR119 and enhances insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8 mM) conditions.
S0080 SNAP94847 hydrochloride SNAP 94847 hydrochloride is a high affinity and selective antagonist of the MCH1 receptor with an IC50 of 230 nM for rat MCH1 in FLIPR calcium mobility assay.
S0083 DJ-V-159 DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
E0377 CLP-3094 CLP-3094, a potent inhibitor targeting the binding function 3 (BF3) site of androgen receptor (AR), inhibits AR transcriptional activity with IC50 of 4 μM, also is a selective, potent GPR142 antagonist.
S0110 APD597 APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
S6759 TC-G-1008 (GPR39-C3) TC-G-1008 (GPR39-C3) is a potent and orally available G-protein coupled receptor 39 (GPR39)(zinc receptor) agonist with EC50 of 0.4 nM and 0.8 nM for rat and human receptors, respectively.
S6425 JNJ 63533054 JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.
E0106 ML401 ML401, a potent chemical probe, selectively antagonizes G-protein coupled receptor 183 (GPR183, EBI2) with an IC50 of 1.03 nM, and displays activity in a chemotaxis assay with IC50 of 6.24 nM.
S0156 CID 1375606 CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.
S6850 NE 52-QQ57 NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
Exp Hematol Oncol, 2024, 13(1):13
S2822 OC000459 OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2.
S0183 NIBR189 NIBR189 is a potent antagonist of the Epstein-Barr virus-induced gene 2 (EBI2, GPR183) receptor with IC50 of 16 nM for binding and 11 nM for function, respectively.
S0851 G-1 (LNS 8801) G-1 (LNS 8801) is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.
iScience, 2024, 27(3):109125
S4709 Latanoprost Latanoprost (Xalatan, PhXA41) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure.
S2954 4-CMTB 4-CMTB is a selective allosteric agonist of free fatty acid receptor 2(FFA2, GPR43) with pEC50 of 6.38.
E2660 Pamoic acid disodium Pamoic acid disodium, a potent GPR35 agonist with an EC50 value of 79 nM, induces GPR35a internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively, also potently recruits β-arrestin2 to GPR35 showing an antinociceptive effect.
S4440 2-Phenylacetamide 2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells.
S3451 PH-064 PH-064 (BIM-46187) is a novel imidazo-pyrazine derivative that inhibits the heterotrimeric G-protein complex effectively. PH-064 (BIM46174) inhibits heterotrimeric G-protein signalling in GPCRsthat mediate cyclic AMP generation (GAs), calcium release (GAq), cancer cell invasion by Wnt-2 frizzled receptors, and high-affinity neurotensin receptors (GAo/i and GAq).
S2637 Fasiglifam(TAK-875) Hemihydrate Fasiglifam(TAK-875) Hemihydrate is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.
Endocrinology, 2021, 162(3)bqab002
Psychopharmacology (Berl), 2021, 10.1007/s00213-021-05837-4
Environ Sci Technol, 2020, 54(6):3428-3436
S8014 GW9508 GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner.
J Enzyme Inhib Med Chem, 2021, 36(1):1651-1658
Bioorg Chem, 2020, 99:103830
Arch Pharm (Weinheim), 2020, e2000275
S8673 ONC212 ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.
OPARU, 2023, 10.18725/OPARU-48122
Pharmacol Res Perspect, 2022, 10(4):e00993
Front Pharmacol, 2021, 12:737637
S6889 Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
Cell Cycle, 2022, 1-11.
Aging (Albany NY), 2021, 13(13):17097-17117
S2149 GSK1292263 GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.
PLoS One, 2015, 10(7):e0134051
S5400 3-chloro-5-hydroxybenzoic Acid 3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81.
MedComm (2020), 2023, 4(2):e242
MedComm (2020), 2023, 4(2):e242
Antioxidants (Basel), 2023, 12(12)2087
S0208 6-OAU 6-OAU (GTPL5846, 6-n-octylaminouracil) is a surrogate agonist of G protein-coupled receptor 84 (GPR84) that activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with EC50 of 105 nM in the PI assay. 6-OAU (GTPL5846, 6-n-octylaminouracil) increases [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with EC50 of 512 nM.
J Orthop Surg Res, 2023, 18(1):3
S0001 GSK137647A GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
S6976 TC-O 9311 TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM.
S6746 APD668 APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
E0347 AS1269574 AS 1269574, a small-molecule G protein-coupled receptor 119 (GPR119) agonist, has an EC50 of 2.5 μM in HEK293 cells transiently expressing human GPR119 and enhances insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8 mM) conditions.
S0083 DJ-V-159 DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
S0110 APD597 APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
S6759 TC-G-1008 (GPR39-C3) TC-G-1008 (GPR39-C3) is a potent and orally available G-protein coupled receptor 39 (GPR39)(zinc receptor) agonist with EC50 of 0.4 nM and 0.8 nM for rat and human receptors, respectively.
S6425 JNJ 63533054 JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.
S0156 CID 1375606 CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.
S4709 Latanoprost Latanoprost (Xalatan, PhXA41) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure.
S2954 4-CMTB 4-CMTB is a selective allosteric agonist of free fatty acid receptor 2(FFA2, GPR43) with pEC50 of 6.38.
E2660 Pamoic acid disodium Pamoic acid disodium, a potent GPR35 agonist with an EC50 value of 79 nM, induces GPR35a internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively, also potently recruits β-arrestin2 to GPR35 showing an antinociceptive effect.
S3451 PH-064 PH-064 (BIM-46187) is a novel imidazo-pyrazine derivative that inhibits the heterotrimeric G-protein complex effectively. PH-064 (BIM46174) inhibits heterotrimeric G-protein signalling in GPCRsthat mediate cyclic AMP generation (GAs), calcium release (GAq), cancer cell invasion by Wnt-2 frizzled receptors, and high-affinity neurotensin receptors (GAo/i and GAq).
S4440 2-Phenylacetamide 2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells.
S6651 G15 G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.
iScience, 2024, 27(3):109125
Nutrients, 2023, 16(1)38
Chem Biol Interact, 2023, 10.1016/j.cbi.2023.110728
S9477 AH7614 AH7614 (compound 39) is a selective FFA4 (GPR120) antagonist with pIC50s of 7.1 for human FFA4 and 8.1 for mouse FFA4.
Cell Prolif, 2023, e13551.
Cell Death Differ, 2021, 10.1038/s41418-021-00887-9
S0135 JMS-17-2 JMS-17-2 is a potent and selective small-molecule antagonist of CX3C chemokine receptor 1 (CX3CR1/GPR13) with IC50 of 0.32 nM. JMS-17-2 is used in the research of metastatic disease in breast cancer patients.
Int J Oncol, 2022, 60(4)47
Brain Res Bull, 2021, S0361-9230(21)00289-6
S7263 AZD1981 AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2.
Mol Cancer Ther, 2019, 18(11):2097-2110
E1235 NF-56-EJ40 NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.
S0742 DC260126 DC260126, a small organic antagonist for GPR40 (FFAR1), dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50=6.28, 5.96, 7.07, 4.58 μM, respectively), reduces GTP-loading and ERK1/2 phosphorylation stimulated by linoleic acid in GPR40-CHO cells, suppresses palmitic acid potentiated glucose-stimulated insulin secretion, and negatively regulates GPR40 mRNA expression induced by oleic acid in Min6 cells.
S0080 SNAP94847 hydrochloride SNAP 94847 hydrochloride is a high affinity and selective antagonist of the MCH1 receptor with an IC50 of 230 nM for rat MCH1 in FLIPR calcium mobility assay.
E0377 CLP-3094 CLP-3094, a potent inhibitor targeting the binding function 3 (BF3) site of androgen receptor (AR), inhibits AR transcriptional activity with IC50 of 4 μM, also is a selective, potent GPR142 antagonist.
E0106 ML401 ML401, a potent chemical probe, selectively antagonizes G-protein coupled receptor 183 (GPR183, EBI2) with an IC50 of 1.03 nM, and displays activity in a chemotaxis assay with IC50 of 6.24 nM.
S6850 NE 52-QQ57 NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
Exp Hematol Oncol, 2024, 13(1):13
S2822 OC000459 OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2.
S0183 NIBR189 NIBR189 is a potent antagonist of the Epstein-Barr virus-induced gene 2 (EBI2, GPR183) receptor with IC50 of 16 nM for binding and 11 nM for function, respectively.
S0851 G-1 (LNS 8801) G-1 (LNS 8801) is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.
iScience, 2024, 27(3):109125
S2637 Fasiglifam(TAK-875) Hemihydrate Fasiglifam(TAK-875) Hemihydrate is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.
Endocrinology, 2021, 162(3)bqab002
Psychopharmacology (Berl), 2021, 10.1007/s00213-021-05837-4
Environ Sci Technol, 2020, 54(6):3428-3436
S8014 GW9508 GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner.
J Enzyme Inhib Med Chem, 2021, 36(1):1651-1658
Bioorg Chem, 2020, 99:103830
Arch Pharm (Weinheim), 2020, e2000275
S8673 ONC212 ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.
OPARU, 2023, 10.18725/OPARU-48122
Pharmacol Res Perspect, 2022, 10(4):e00993
Front Pharmacol, 2021, 12:737637
S6889 Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
Cell Cycle, 2022, 1-11.
Aging (Albany NY), 2021, 13(13):17097-17117
S2149 GSK1292263 GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.
PLoS One, 2015, 10(7):e0134051
S5400 3-chloro-5-hydroxybenzoic Acid 3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81.
MedComm (2020), 2023, 4(2):e242
MedComm (2020), 2023, 4(2):e242
Antioxidants (Basel), 2023, 12(12)2087
S0208 6-OAU 6-OAU (GTPL5846, 6-n-octylaminouracil) is a surrogate agonist of G protein-coupled receptor 84 (GPR84) that activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with EC50 of 105 nM in the PI assay. 6-OAU (GTPL5846, 6-n-octylaminouracil) increases [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with EC50 of 512 nM.
J Orthop Surg Res, 2023, 18(1):3
S0001 GSK137647A GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
S6976 TC-O 9311 TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM.
S6746 APD668 APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
E0347 AS1269574 AS 1269574, a small-molecule G protein-coupled receptor 119 (GPR119) agonist, has an EC50 of 2.5 μM in HEK293 cells transiently expressing human GPR119 and enhances insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8 mM) conditions.
S0083 DJ-V-159 DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
S0110 APD597 APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
S6759 TC-G-1008 (GPR39-C3) TC-G-1008 (GPR39-C3) is a potent and orally available G-protein coupled receptor 39 (GPR39)(zinc receptor) agonist with EC50 of 0.4 nM and 0.8 nM for rat and human receptors, respectively.
S6425 JNJ 63533054 JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.
S0156 CID 1375606 CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.
S4709 Latanoprost Latanoprost (Xalatan, PhXA41) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure.
S2954 4-CMTB 4-CMTB is a selective allosteric agonist of free fatty acid receptor 2(FFA2, GPR43) with pEC50 of 6.38.
E2660 Pamoic acid disodium Pamoic acid disodium, a potent GPR35 agonist with an EC50 value of 79 nM, induces GPR35a internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively, also potently recruits β-arrestin2 to GPR35 showing an antinociceptive effect.

GPR阻害剤の選択性比較

Tags: GPR inhibitor|GPR agonist|GPR activator|GPR inducer|GPR antagonist|GPR signaling pathway|GPR assay kit