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
T1237	Azathioprine	Azathioprine, an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.
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.
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.
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...
T4312	GPR120 receptor agonist	A potent and selective GPR120 receptor 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.
T4626	TC-O 9311	TC-O 9311 is a potent GPR139 agonist.
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.
T7261	Grp94 Inhibitor-1	Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor (IC50 : 2 nM).
T7127	DC260126	DC260126 is a small-molecule antagonist of FFA1 (GPR40)
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, an...
T7482	3-chloro-5-hydroxybenzoic Acid	3-chloro-5-hydroxy Benzoic Acid (3-chloro-5-hydroxy BA) is an agonist of GPR81 (EC50 : 16 M)
T7713	Benzyl nicotinate	Benzyl Nicotinate is a agonist of GPR109A receptor and GPR109B receptor
TQ0020	AMG 837 calcium hydrate	AMG 837 calcium hydrate is a potent GPR40 agonist(EC50: 13 nM) with highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM).
TQ0051	MK-7246	MK-7246 is a potent and specific CRTH2 antagonist (Ki: 2.5 nM).
TQ0108	MK-6892	MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).
TQ0241	TUG-770	TUG-770 is a highly potent agonist of free fatty acid receptor 1 (FFA1/GPR40, EC50: 6 nM for hFFA1).
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 ...
T8353	Pamoic acid	Pamoic acid is the orphan G protein-coupled receptor GPR35 agonist. Pamoic acid activates ERK and beta-arrestin2 and causes antinociceptive activity.
TN2268	Tetrahydromagnolol	Tetrahydromagnolol can activate cannabinoid (CB) receptors.
T8329	AR 231453	AR 231453 is a selective and orally available GPR119 agonist,can stimulate β-cell replication and improve islet graft function.
T12216	NF-56-EJ40	NF-56-EJ40 is a high-affinity and highly selective antagonist of human SUCNR1 (GPR91) (IC50 of 25 nM).
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...
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...
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).
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...
T10691	CAY10595	CAY10595 is a potent antagonist of the CRTH2/DP2 receptor (Ki: 10 nM).
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.
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.
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.
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...
TP2165	Urotensin II, mouse acetate	Urotensin II, mouse acetate is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.
TP2166	Urotensin II, mouse TFA	Urotensin II, mouse TFA is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.
T12778L	RTI-13951-33	RTI-13951-33 is an effective and brain-penetrant GPR88 agonist (EC50: 25 nM, in GPR88 cAMP functional assay).
T5036	cangrelor tetrasodium	Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.