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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC79784 Zelandopam anhydrous
Zelandopam (anhydrous) (YM435 (anhydrous)) is an orally active and selective agonist of the dopamine D1 receptor. Zelandopam (anhydrous) possesses potent renal vasodilatory properties and can effectively alleviate Cisplatin-induced acute renal failure.
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DC79783 AM11542
AM11542 is a orthosteric agonist of cannabinoid receptor 1 (CB1), with a reported binding affinity (Ki) of 0.11 nM. AM11542 can be used for the study of CB1 receptor activation and related allosteric modulation mechanisms.
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DC79780 (S)-SCH-23390 hydrochloride
(S)-SCH-23390 (hydrochloride) is the S-enantiomer of SCH-23390. SCH-23390 is a dopamine D1-like receptor antagonist (with Ki values of 0.2 nM and 0.3 nM for the D1 and D5 receptor subtypes, respectively).
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DC79768 MRS2690 disodium
MRS2690 disodium is a selective P2Y14 receptor agonist. MRS2690 disodium inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 disodium induces intracellular calcium mobilization, activates P38 and stimulates [35S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690 disodium can be used for ischemic heart disease.
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DC79761 K-833
K-833 is a GPR119 agonist with EC50 values of 39.8 nM (human), 100nM (mouse), 75.4 nM (rat) and 12.6 nM (dog). K-833 demonstrates a modest increase in GLP-1 secretion and leads to a synergistic increase in GLP-1 levels when combined with AM-5262 in acute gut peptide secretion assays in mice. K-833 can be used in studies on weight loss.
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DC79760 CI-988 meglumin
CI-988 (meglumin) is a cholecystokinin 2 receptor (CCK2R) antagonist. CI-988 (meglumin) prevents the gastrin-mediated protection of the heart with ischemia/reperfusion injury.
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DC79757 TKS 159
TKS 159 is a 5-HT4 receptor agonist. TKS 159 can promote gastrointestinal motility. TKS 159 can be used for research on gastrointestinal conditions.
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DC79750 MDL 43291
MDL 43291 is a competitive leukotriene (LT) receptor antagonist. MDL 43291 antagonize LTD4 and LTE4 with pA2 of 6.7. MDL 43291 does not antagonize histamine, carbachol or substance P. MDL 43291 can be used for the researches of inflammation and immunology, such as asthma.
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DC79735 PD 121981
PD 121981 is a angiotensin II receptor antagonist. PD 121981 can be used for the research of cardiovascular disease.
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DC79731 VUF26034
VUF26034 (Compound 12b) is a photoresponsive ligand for the human β2-adrenergic receptor (β2-AR.
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DC79728 S-1255
S-1255 is an orally active and highly selective endothelin ETA receptor antagonist (Kd=0.39 nM). S-1255 blocks vasoconstriction and sustains hypotensive effects in hypertensive rats. S-1255 is promising for research of hypertension and cardiovascular disorders.
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DC79724 TGI-15
TGI-15 is a highly selective prostaglandin F receptor antagonist. TGI-15 inhibits downstream signaling pathways by blocking the binding of PGF2 α to FP receptors. TGI-15 can be used for research on fibrotic and inflammatory conditions.
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DC79723 BMT-136088
BMT-136088 is a radioligand used for positron emission tomography (PET) imaging of idiopathic pulmonary fibrosis.
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DC79717 CGP 57698
CGP 57698 is an efficient CysLT receptor (Ki = 5.7 nM) antagonist. CGP 57698 can effectively counteract bronchoconstriction caused by LTD4. CGP 57698 can be used for research on asthma or allergic conditions.
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DC79709 LY459477
LY459477 is a potent, selective and orally active metabotropic glutamate 2/3 receptor (mGluR2/3) agonist. LY459477 can effectively suppress Phencyclidine-evoked locomotor activity at doses that do not impair neuromuscular coordination. LY459477 can be used for the research of neurological disease.
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DC79692 LMD-902
LMD-902, a LMD-009) analog, is a CCR8 agonist with an EC50 of 15  nM. LMD-902 has a superior binging capacity depending on key residues such as PheVI:16. LMD-902 can be used for inflammation diseases like bronchial asthma and central nervous system diseases like multiple sclerosis research.
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DC79691 Diosuxentan
Diosuxentan is an inhibitor of ETA. Diosuxentan can be used in research for cardiovascular, renal and neuronal inflammation diseases.
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DC79690 ABT-866
ABT-866 is an α1A-adrenoceptor agonist and an antagonist at the α1B- and α1D-adrenoceptor subtypes. ABT-866 has an EC50 of 0.60 μM for the α1A in the rabbit urethra. ABT-866 has a pA2 value of 5.4 for the α1B in the rat spleen. ABT-866 has a pA2 value of 6.2 for the α1D in the rat aorta. ABT-866 exhibits good urethral selectivity and lower cardiovascular side effects in stress urinary incontinence models. ABT-866 can be used for the research of diseases such as stress urinary incontinence.
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DC79683 UK-224671
UK-224671 is a potent and selective NK2 receptor antagonist. UK-224671 is affected by P-gp efflux and poor intrinsic membrane permeability, resulting in low oral bioavailability.
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DC79678 SB 258741
SB 258741 is an efficient and highly selective 5-HT7 receptor (pKi = 8.
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DC79671 BMS-187308
BMS-187308 is an orally active endothelin-A (ETA) antagonist, with Kis of 4.7 nM for ETA and 1.7 μM for ETB. BMS-187308 inhibits the pressor response to ET-1 (ED25: 1.2 µmol/kg; iv). BMS-187308 is a suitable tool for investigating the role of endothelin.
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DC79662 L742791
L742791 is a β3-AR agonist. L742791 elicits lipolytic response in isolated nonhuman primate adipocytes.
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DC79661 PF-04363467
PF-04363467 is a highly preferring D3R antagonist. PF-04363467 produces dose-dependent changes in the EEG profile of freely moving rats. PF-4363467 attenuates opioid drug-seeking behavior without concomitant D2 side effects. PF-04363467 can be used for the study of addiction, cognitive and mental illness.
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DC79659 BVT-74316
BVT-74316 is a 5-HT6 receptor antagonist. BVT-74316 can reduce food intake and bodyweight gain in rodent models. BVT-74316 can be used for the research of metabolic disease, such as obesity.
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DC79658 GG-818
GG-818 is a potent and selective α1 adrenoceptor antagonist, with pKi values of 9.7 for α1a, 7.8 for α1b, and 7.6 for α1d. GG-818 can be used for benign prostatic hyperplasia research.
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DC79640 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA
1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA is a phospholipid containing arachidonic acid at the sn-1 position. It is a precursor to 1-arachidonoyl glycerol (1-Monoarachidin). 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM. It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS. It also decreases differentiation of HT-29 human colon carcinoma cells to goblet cells in the presence of sodium butyrate.
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DC79632 A-72055
A-72055 is a partial agonist of muscarinic receptors. A-72055 has binding activity to both M1 and M2 receptors, with Ki values of 32 nM and 30 nM, respectively. A-72055 can enhance cognitive function and improve learning and memory deficits. A-72055 has better security. A-72055 can be used for research on neurological disorders such as cognitive impairment.
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DC79621 Batoprazine
Batoprazine (8-(1-piperazinyl)-2H-1-benzopyran-2-one)) is a 5-HT1A,1B receptor agonist. Batoprazine can replace the behavioral stimulus of eltoprazine in the two-lever operant discrimination test between eltoprazine and deionized water in rats (ED50: 0.20 mg/kg).
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DC79619 AGN192093
AGN192093 is a TP agonist (EC50 = 1.3 nM). AGN192093 exhibits potent and selective thromboxane analog activity in rat blood vessels.
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DC79614 GSK-163090 dihydrochloride
GSK-163090 (dihydrochloride) is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4, 8.5 and 9.7, respectively. GSK-163090 (dihydrochloride) inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK-163090 (dihydrochloride) has antidepressant and anxiolytic activities.
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