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.