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GPR
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 nM in the PI assay.
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 JNJ63533054 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 TUG891 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 acids.
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 by the mast cells an
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, including DP1. AZD
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 that developed resis
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-fold selectivity over H
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, and >10,000 nM,respect
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 nM).
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-proliferative actions.
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 not inhibit GPR110
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, respectively.
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 actions.
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-carboxylic acid recept
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 of Ipomoea muricata
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.
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