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Focused Bioactive Libraries General Bioactive Libraries Approved / Repurposing Disease Focused Target / Pathway Focused Characteristic Bioactive Libraries
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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 CAS No. Purity Chemical Structure
T12375 Fezagepras sodium 1254472-97-3 98%
Fezagepras sodium is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferati...
T10889 CRTh2 antagonist 2 780763-95-3 98%
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.
T27328 FL104 885672-81-1 98%
FL104 is a potent agonist of small-molecule urotensin II receptor, pEC50= 7.11.
T67892 BTB09089 245728-44-3 98%
BTB09089 is a T cell death-associated gene 8 (TDAG8/GPR65)-specific agonist.BTB09089 induces TDAG8 expression and regulates cytokine production in T cells and ma...
T23434 GPR35 agonist 2 494191-73-0 98%
GPR35 agonist 2 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.
T11411 GLPG1205 1445847-37-9 98%
GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and ...
T67791 BMS-903452 1339944-47-6 98%
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 wa...
TQ0241 TUG-770 1402601-82-4 98%
TUG-770 is a highly potent agonist of free fatty acid receptor 1 (FFA1/GPR40, EC50: 6 nM for hFFA1).
T10507 GPR40 Agonist 2 1147729-48-3 98%
GPR40 Agonist 2 is a GPR40 agonist extracted from patent WO2009054479A1. It can be used in the research of diabetes.
T11044 Dihydromunduletone 674786-20-0 98%
Dihydromunduletone (DHM) is a carotenoid derivative and selective strong adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonists, does ...
T4689 Palosuran hydrochloride 540769-28-6(free base） T4689 98%
Palosuran is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.
T15283 Firuglipel 1371591-51-3 98%
Firuglipel is an orally available and selective agonist of GPR119.
T14200 AM-1638 1142214-62-7 98%
AM-1638 is a full agonist of GPR40/FFA1 (EC50: 0.16 μM).
T14202 AM-4668 1011531-27-3 98%
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, respec...
T15448 GW-1100 306974-70-9 98%
GW-1100 is a selective antagonist of GPR40 (pIC50: 6.9). GW1100 also plays the role of a GPR40 inverse agonist.
T2351L TAK-875 Hemihydrate 1374598-80-7 98%
TAK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid.
T11452 GPR120 Agonist 1 1628448-77-0 98%
GPR120 Agonist 1 is a selective GPR120 agonist. In GPR120 transfected HEK293 cells, GPR120 Agonist 1 displays good EC50 of 42 nM and 77 nM for human and mouse GP...
T11460 GPR4 antagonist 1 1197879-16-5 98%
GPR4 antagonist 1 is a GPR4 antagonist (IC50: 189 nM).
TP2166 Urotensin II, mouse TFA (9047-55-6 free base) TP2166 98%
Urotensin II, mouse TFA is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.
T12778L RTI-13951-33 2244884-08-8 98%
RTI-13951-33 is an effective and brain-penetrant GPR88 agonist (EC50: 25 nM, in GPR88 cAMP functional assay).
Fezagepras sodium
T12375
Fezagepras sodium is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferati...
CRTh2 antagonist 2
T10889
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.
FL104
T27328
FL104 is a potent agonist of small-molecule urotensin II receptor, pEC50= 7.11.
BTB09089
T67892
BTB09089 is a T cell death-associated gene 8 (TDAG8/GPR65)-specific agonist.BTB09089 induces TDAG8 expression and regulates cytokine production in T cells and ma...
GPR35 agonist 2
T23434
GPR35 agonist 2 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.
GLPG1205
T11411
GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and ...
BMS-903452
T67791
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 wa...
TUG-770
TQ0241
TUG-770 is a highly potent agonist of free fatty acid receptor 1 (FFA1/GPR40, EC50: 6 nM for hFFA1).
GPR40 Agonist 2
T10507
GPR40 Agonist 2 is a GPR40 agonist extracted from patent WO2009054479A1. It can be used in the research of diabetes.
Dihydromunduletone
T11044
Dihydromunduletone (DHM) is a carotenoid derivative and selective strong adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonists, does ...
Palosuran hydrochloride 540769-28-6(free base）
T4689
Palosuran is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.
Firuglipel
T15283
Firuglipel is an orally available and selective agonist of GPR119.
AM-1638
T14200
AM-1638 is a full agonist of GPR40/FFA1 (EC50: 0.16 μM).
AM-4668
T14202
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, respec...
GW-1100
T15448
GW-1100 is a selective antagonist of GPR40 (pIC50: 6.9). GW1100 also plays the role of a GPR40 inverse agonist.
TAK-875 Hemihydrate
T2351L
TAK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid.
GPR120 Agonist 1
T11452
GPR120 Agonist 1 is a selective GPR120 agonist. In GPR120 transfected HEK293 cells, GPR120 Agonist 1 displays good EC50 of 42 nM and 77 nM for human and mouse GP...
GPR4 antagonist 1
T11460
GPR4 antagonist 1 is a GPR4 antagonist (IC50: 189 nM).
Urotensin II, mouse TFA (9047-55-6 free base)
TP2166
Urotensin II, mouse TFA is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.
RTI-13951-33
T12778L
RTI-13951-33 is an effective and brain-penetrant GPR88 agonist (EC50: 25 nM, in GPR88 cAMP functional assay).
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