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Endocrinology/Hormones GPR

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
T10084 CRTh2 antagonist 1 CRTh2 antagonist 1 is a CRTh2 antagonist (IC50: 89 nM).
T10507 GPR40 Agonist 2 GPR40 Agonist 2 is a GPR40 agonist extracted from patent WO2009054479A1. It can be used in the research of diabetes.
T10691 CAY10595 CAY10595 is a potent antagonist of the CRTH2/DP2 receptor (Ki: 10 nM).
T10889 CRTh2 antagonist 2 CRTh2 antagonist selective and potent CRTH2 antagonist, IC50≤10 nM. CRTh2 antagonist 2 can be used to study the direction of androgenic alopecia.
T11044 Dihydromunduletone Dihydromunduletone (DHM) is a carotenoid derivative and selective strong adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonists, does...
T11452 GPR120 Agonist 1 GPR120 agonist 1 is an effective and selective GPR120 agonist with good anti-diabetes effect and safety, and is a candidate drug.
T11458 GPR40/FFAR1 modulator 1 GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
T11460 GPR4 antagonist 1 GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM. 
T11461 NE 52-QQ57 NE 52-QQ57 has anti-inflammatory activity. NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. 
T11462 GPR84 antagonist 8 GPR84 antagonist 8 is a selective GPR84 antagonist.
T11560 hGPR91 antagonist 1 HGPR91 antagonist 1 is a potent and selective small molecule hGPR91 antagonist with an IC50 of 7 μM. 
T12216 NF-56-EJ40 NF-56-EJ40 is a high-affinity and highly selective antagonist of human SUCNR1 (GPR91) (IC50 of 25 nM).
T1237 Azathioprine Azathioprine, an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.
T12375 Setogepram sodium salt 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-proli...
T12778L RTI-13951-33 RTI-13951-33 is an effective and brain-penetrant GPR88 agonist (EC50: 25 nM, in GPR88 cAMP functional assay).
T12883 Setogepram Setogepram is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84,with anti-inflammatory, anti-fibroticand anti-proliferative action...
T14200 AM-1638 AM-1638 is a full agonist of GPR40/FFA1 (EC50: 0.16 μM).
T14202 AM-4668 AM-4668 is a type 2 diabetes GPR40 agonist. For GPR40, in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), the EC50s are 3.6 nM and 36 nM, respe...
T15283 Firuglipel Firuglipel is an orally available and selective agonist of GPR119.
T15352 FTBMT FTBMT is a selective GPR52 agonist (EC50: 75 nM) and has antipsychotic and procognitive properties.
T15364 G-1 G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).
T15388 GLPG0974 GLPG0974 is an antagonist of free fatty acid receptor-2 (IC50: 9 nM).
T15432 GSK256073 GSK256073 is a selective and orally active GPR109A (G-protein coupled receptor 109A) agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-ca...
T15448 GW-1100 GW-1100 is a selective antagonist of GPR40 (pIC50: 6.9). GW1100 also plays the role of a GPR40 inverse agonist.
T15824 Lysergol Lysergol has been used as a hypotensive, psychotropic analgesic, and uterus- and intestine-stimulating drug. Lysergol is a clavinet alkaloid isolated from seeds...
T1781 GW 9508 GW9508 is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.
T1793 MBX2982 MBX-2982 is a selective, orally-available GPR119 agonist, used for the treatment of diabetes.
T1915 AM251 AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 ...
T2036 GTPL5846 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...
T2058 Palosuran Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor.
T2088 APD 668 APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.
T2351 TAK875 TAK875 is a potent, selective and orally bioavailable GPR40 agonist.
T2351L TAK-875 Hemihydrate TAK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid.
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.
T2528 Latanoprost Latanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.
T2664 Timapiprant OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist (IC50: 13 nM).
T2701 GSK1292263 GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.
T3119 JNJ-63533054 JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.
T3171 GSK137647A GSK137647A is a selective FFA4 agonist.
T3176 APD597 APD597 is a GPR119 agonist, used in the treatment of type 2 diabetes.
T3433 TUG-891 TUG-891 is a G protein-coupled receptor (GPCR) expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty a...
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 ...
T3965 Fevipiprant Fevipiprant is a selective, potent, reversible competitive CRTh2 antagonist.
T4312 GPR120 receptor agonist A potent and selective GPR120 receptor agonist.
T4626 TC-O 9311 TC-O 9311 is a potent GPR139 agonist.
T4689 Palosuran hydrochloride 540769-28-6(free base) Palosuran is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.
T5828 MS21570 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.
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...
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 ...
T7010 VER155008 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-fol...
CRTh2 antagonist 1
T10084CAS 1379445-54-1
CRTh2 antagonist 1 is a CRTh2 antagonist (IC50: 89 nM).
GPR40 Agonist 2
T10507CAS 1147729-48-3
GPR40 Agonist 2 is a GPR40 agonist extracted from patent WO2009054479A1. It can be used in the research of diabetes.
CAY10595
T10691CAS 916047-16-0
CAY10595 is a potent antagonist of the CRTH2/DP2 receptor (Ki: 10 nM).
CRTh2 antagonist 2
T10889CAS 780763-95-3
CRTh2 antagonist selective and potent CRTH2 antagonist, IC50≤10 nM. CRTh2 antagonist 2 can be used to study the direction of androgenic alopecia.
Dihydromunduletone
T11044CAS 674786-20-0
Dihydromunduletone (DHM) is a carotenoid derivative and selective strong adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonists, does...
GPR120 Agonist 1
T11452CAS 1628448-77-0
GPR120 agonist 1 is an effective and selective GPR120 agonist with good anti-diabetes effect and safety, and is a candidate drug.
GPR40/FFAR1 modulator 1
T11458CAS 874755-26-7
GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
GPR4 antagonist 1
T11460CAS 1197879-16-5
GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM. 
NE 52-QQ57
T11461CAS 1401728-56-0
NE 52-QQ57 has anti-inflammatory activity. NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. 
GPR84 antagonist 8
T11462CAS 1445846-30-9
GPR84 antagonist 8 is a selective GPR84 antagonist.
hGPR91 antagonist 1
T11560CAS 1314796-00-3
HGPR91 antagonist 1 is a potent and selective small molecule hGPR91 antagonist with an IC50 of 7 μM. 
NF-56-EJ40
T12216CAS 2380230-73-7
NF-56-EJ40 is a high-affinity and highly selective antagonist of human SUCNR1 (GPR91) (IC50 of 25 nM).
Azathioprine
T1237CAS 446-86-6
Azathioprine, an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.
Setogepram sodium salt
T12375CAS 1254472-97-3
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-proli...
RTI-13951-33
T12778LCAS 2244884-08-8
RTI-13951-33 is an effective and brain-penetrant GPR88 agonist (EC50: 25 nM, in GPR88 cAMP functional assay).
Setogepram
T12883CAS 1002101-19-0
Setogepram is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84,with anti-inflammatory, anti-fibroticand anti-proliferative action...
AM-1638
T14200CAS 1142214-62-7
AM-1638 is a full agonist of GPR40/FFA1 (EC50: 0.16 μM).
AM-4668
T14202CAS 1011531-27-3
AM-4668 is a type 2 diabetes GPR40 agonist. For GPR40, in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), the EC50s are 3.6 nM and 36 nM, respe...
Firuglipel
T15283CAS 1371591-51-3
Firuglipel is an orally available and selective agonist of GPR119.
FTBMT
T15352CAS 1358575-02-6
FTBMT is a selective GPR52 agonist (EC50: 75 nM) and has antipsychotic and procognitive properties.
G-1
T15364CAS 881639-98-1
G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).
GLPG0974
T15388CAS 1391076-61-1
GLPG0974 is an antagonist of free fatty acid receptor-2 (IC50: 9 nM).
GSK256073
T15432CAS 862892-90-8
GSK256073 is a selective and orally active GPR109A (G-protein coupled receptor 109A) agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-ca...
GW-1100
T15448CAS 306974-70-9
GW-1100 is a selective antagonist of GPR40 (pIC50: 6.9). GW1100 also plays the role of a GPR40 inverse agonist.
Lysergol
T15824CAS 602-85-7
Lysergol has been used as a hypotensive, psychotropic analgesic, and uterus- and intestine-stimulating drug. Lysergol is a clavinet alkaloid isolated from seeds...
GW 9508
T1781CAS 885101-89-3
GW9508 is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.
MBX2982
T1793CAS 1037792-44-1
MBX-2982 is a selective, orally-available GPR119 agonist, used for the treatment of diabetes.
AM251
T1915CAS 183232-66-8
AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 ...
GTPL5846
T2036CAS 83797-69-7
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...
Palosuran
T2058CAS 540769-28-6
Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor.
APD 668
T2088CAS 832714-46-2
APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.
TAK875
T2351CAS 1000413-72-8
TAK875 is a potent, selective and orally bioavailable GPR40 agonist.
TAK-875 Hemihydrate
T2351LCAS 1374598-80-7
TAK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid.
Ramatroban
T2396CAS 116649-85-5
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.
Latanoprost
T2528CAS 130209-82-4
Latanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.
Timapiprant
T2664CAS 851723-84-7
OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist (IC50: 13 nM).
GSK1292263
T2701CAS 1032823-75-8
GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.
JNJ-63533054
T3119CAS 1802326-66-4
JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.
GSK137647A
T3171CAS 349085-82-1
GSK137647A is a selective FFA4 agonist.
APD597
T3176CAS 897732-93-3
APD597 is a GPR119 agonist, used in the treatment of type 2 diabetes.
TUG-891
T3433CAS 1374516-07-0
TUG-891 is a G protein-coupled receptor (GPCR) expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty a...
Setipiprant
T3520CAS 866460-33-5
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 ...
Fevipiprant
T3965CAS 872365-14-5
Fevipiprant is a selective, potent, reversible competitive CRTh2 antagonist.
GPR120 receptor agonist
T4312CAS 1234844-11-1
A potent and selective GPR120 receptor agonist.
TC-O 9311
T4626CAS 444392-31-4
TC-O 9311 is a potent GPR139 agonist.
Palosuran hydrochloride 540769-28-6(free base)
T4689CAS T4689
Palosuran is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.
MS21570
T5828CAS 65373-29-7
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.
AZD1981
T6399CAS 802904-66-1
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...
HA15
T6855CAS 1609402-14-3
HA15 targets specifically BiP/GRP78/HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells ...
VER155008
T7010CAS 1134156-31-2
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-fol...