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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC70823 TAK-925 Featured
TAK-925 (Danavorexton) is a potent, selective, and brain-penetrant Orexin 2 receptor (OX2R) agonist with EC50 of 5.5 nM, no significant inhibition on OX1R (IC50>100 uM).TAK-925 also showed good selectivity against 106 off-target enzymes and receptors.
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DC71032 DS-3801b Featured
DS-3801b is a potent and non-macrolide agonist of GPR38. DS-3801b is expected to be novel gastrointestinal prokinetic agents for the research of functional gastrointestinal disorders such as gastroparesis and chronic constipation.
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DC72339 PF-07258669 Featured
PF-07258669 is a melanocortin-4 receptor (MC4) antagonist. PF-07258669 can be used for the research of cachexia, anorexia, or anorexia nervosa.
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DC9508 CPPHA Featured
CPPHA is a selective positive allosteric modulator of mGluR5 receptor.
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DC72820 Macimorelin acetate
Macimorelin (EP-1572) acetate, a GH secretagogue, is an orally active GHSR agonist. Macimorelin acetate stimulates GH release. Macimorelin acetate can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS).
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DC28234 L-803087 Featured
L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM, which is > 280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.
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DC46145 Paltusotine Featured
Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.
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DC40760 Salmeterol-D3
Salmeterol-D3 is the deuterium labeled Salmeterol. Salmeterol is a long-acting beta2-adrenergic receptor agonist that is used for the study of asthma and chronic obstructive pulmonary disease (COPD).
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DC72007 (3R,5R,6S)-Atogepant
(3R,5R,6S)-Atogepant ((3R,5R,6S)-MK-8031) is the enantiomer of Atogepant. Atogepant is a calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.
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DC46241 GPR40/FFAR1 modulator 1(WUN55267) Featured
GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
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DC72641 ONO-0740556
ONO-0740556 is a potent Gi-coupled human lysophosphatidic acid receptor 1 (LPA1) agonist with an EC50 value of 0.26 nM.
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DC72640 Fingolimod phosphate
Fingolimod phosphate (FTY720 phosphate) is an orally active sphingosine 1-phosphate (S1P) receptor agonist. Fingolimod phosphate can promote the neuroprotective effects of microglia. Fingolimod phosphate can be used for the research of multiple sclerosis and neurologic diseases.
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DC72639 I-SAP
I-SAP is a radioiodinated TXA2/PGH2 receptor antagonist. The bind between I-SAP and the receptors, is inhibited by the histidine modifying reagent diethyl-pyrocarbonate (DEPC).
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DC72638 AL-3138
AL-3138 (11-Deoxy-16-fluoro PGF2α) is a prostaglandin F2 alpha (PGF2alpha) analogue that antagonises FP prostaglandin receptor-mediated inositol phosphate production.
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DC72637 AS604872
AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour.
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DC72636 Thromboxane A2
Thromboxane A2 (TXA2) is a prostanoid mediator produced by the metabolism of Arachidonic acid through the cyclooxygenase pathway. Thromboxane A2 activates the thromboxane-prostanoid (TP) receptors. Thromboxane A2 is a potent vasoconstrictor eicosanoid. Thromboxane A2 (TXA2) leads to potent vasoconstriction by stimulation of smooth muscle cells. Thromboxane A2 acts as s tonic immunoregulator to regulate adaptive immune responses.
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DC72635 SC 51089 free base
SC 51089 free base is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity.
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DC72633 Naloxonazine
Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function.
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DC72632 (S,S)-J-113397
(S,S)-J-113397 is an isomer of J-113397. J-113397 is an Opioid Receptor antagonist.
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DC72631 MTEP
MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research.
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DC72630 L-CCG-I
L-CCG-I is an extended isomer of conformationally restricted glutamate analog. L-CCG-I also is a potent agonist for mGluR2 with an EC50 value of 0.3 nM. L-CCG-I can be used for the research of mGluR family.
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DC72628 Afacifenacin
Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB).
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DC72627 PTAC oxalate
PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects.
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DC72626 ST-1006
ST-1006 is a potent histamine H4 receptor agonist with a pKi value of 7.94. ST-1006 has anti-inflammatory effect.
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DC72625 Immepip
Immepip is a H3 agonist. Immepip can reduce cortical histamine release. Immepip can be used for the research of neurological diseases.
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DC72624 LP-471756
LP-471756 is a potent GPR139 antagonist with an IC50 value of 640 nM. LP-471756 inhibits LP-360924-stimulated cAMP production.
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DC72623 PAOPA
PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the high affinity dopamine D2 receptor and promotes its binding to agonists.
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DC72622 PD 168568
PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research.
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DC72621 Pirnabine
Pirnabine is a cannabinoid receptor ligand. Pirnabine can be used for the research of glaucoma.
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DC72620 GW 833972A
GW 833972A is a selective CB2 receptor agonist. GW 833972A inhibits induced nerve depolarization and citric acid-induced cough in animal models.
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