Melatonin Receptor
Melatonin receptors belong to the G protein-coupled receptor superfamily, which preferentially couple to Gαi/o proteins. The melatonin receptor subfamily is composed of three members in mammals: MT1 and MT2, which are both binding to the neurohormone melatonin with high affinity, and GPR50, which shows high sequence homology to MT1 and MT2 but does not bind to melatonin or any other known ligand.
MT1 and MT2 are involved in various biological functions including the regulation of biological rhythms, sleep, pain, retinal, neuronal and immune functions. Alteration of melatonin receptor function or expression in humans is associated with depression, Alzheimer’s disease and type 2 diabetes.
Melatonin Receptor Isoform Specific Products
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Melatonin Receptor Inhibitors
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Melatonin Receptor Agonists
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Melatonin Receptor Antagonists
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Melatonin Receptor Activators
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Melatonin Receptor Modulator
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Melatonin Receptor Control
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Melatonin Receptor Related Products (66)
Related Products (66)
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Melatonin Receptor Isoform Comparison
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Ramelteon metabolite M-II
0 ImagesRamelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist.
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Agomelatine-d6
0 ImagesSynonyms: S-20098-d6
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Cyclo(L-leucyl-L-tryptophyl)
0 ImagesSynonyms: Cyclo(Leu-Trp)Cyclo(L-leucyl-L-tryptophyl) (Cyclo(-Leu-Trp)) is a cyclic dipeptide that inhibits a various of bacteria and fungi. Cyclo(L-leucyl-L-tryptophyl) is a melatonin receptor agonist and is also used as a bitter ligand.
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CGP52608
0 ImagesCGP52608 is a selective agonist for the RZR/ROR receptor, known for its anti-tumor activity, and has almost no affinity for the cell surface G-protein coupled melatonin receptor. CGP52608 can inhibit the growth of mouse 16/C breast cancer cells. CGP52608 can induce the formation of vesicles in diatoms.
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Ramelteon-d5
0 ImagesCat. No.: HY-A0014SCAS No.: 1134159-63-9Synonyms: TAK-375-d5Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.
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Agomelatine-d3
0 ImagesSynonyms: S-20098-d3Agomelatine-d3 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
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S-20928
0 ImagesS-20928 is an antagonist for melatonin receptor through inhibition of binding of melatonin to its receptors. S-20928 enhances the 2-Deoxy-D-glucose (2DG) (HY-13966)-induced increase in blood glucose and glucagon levels in rats brain.
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Agomelatine (Standard)
0 ImagesSynonyms: S-20098 (Standard)Agomelatine (Standard) is the analytical standard of Agomelatine. This product is intended for research and analytical applications. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
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N-Pentanoyl 2-benzyltryptamine
0 ImagesN-Pentanoyl 2-benzyltryptamine is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. N-Pentanoyl 2-benzyltryptamine shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. N-Pentanoyl 2-benzyltryptamine can inhibit melatonin-induced enhancement of electrically-evoked responses.
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Agomelatine-d4
0 ImagesCat. No.: HY-17038S1CAS No.: 1079389-44-8Synonyms: S-20098-d4Agomelatine-d4 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
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Melatonin receptor agonist 1
0 ImagesCat. No.: HY-147542CAS No.: 2411150-76-8Melatonin receptor agonist 1 (compound 20c) is a potent melatonin receptor (MT) agonist, with Ki values of 108 nM (MT2) and 1140 nM (MT1).
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UCM1400
0 ImagesCat. No.: HY-180198UCM1400 is a melatonin receptor (MT) subtype-selective modulator. UCM1400 shows agonistic effect for MT1 and antagonistic effect for MT2 with pKi values of 7.94 and 8.11. UCM1400 can inhibit the decrease in cAMP mediated by the MT2 receptor with a pIC50 of 7.87. UCM1400 exhibits anti-proliferative activity against human glioma cells and inhibit tumor growth. UCM1400 can be used for the research of cancer, such as glioma.
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UCM 549
0 ImagesCat. No.: HY-119010CAS No.: 753502-19-1
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5-MCA-NAT
0 ImagesCat. No.: HY-101303CAS No.: 190277-13-55-MCA-NAT is a melatonin agonist that may target the melatoninMT3 receptor. 5-MCA-NAT can contract the colonic band in a concentration-dependent manner and reduce intraocular pressure (IOP) in glaucomatous monkey eyes, inhibiting the increase in IOP.
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7-Desmethyl-3-hydroxyagomelatine
0 ImagesCat. No.: HY-133112CAS No.: 166527-00-0Synonyms: 3-Hydroxy-7-desmethyl agomelatine
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UCM 793
0 ImagesCat. No.: HY-115304CAS No.: 101374-18-9UCM 793 is a non-selective MT1/MT2 receptor agonist (pKis: 9.09 (MT1 receptor); 9.19 (MT2 receptor)). UCM793 increases the number of episodes and decreases the length of the episodes of wakefulness. UCM 793 influences quality of the vigilance states. UCM 793 decreases sleep onset without having an effect on NREM sleep maintenance.
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Melatonin-Tamoxifen Conjugate
0 ImagesCat. No.: HY-169382Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate composed of Melatonin (HY-B0075) and Tamoxifen (HY-13757A), which is a potent antagonist of ERα (IC50=863 nM). Melatonin-Tamoxifen Conjugate binds to MLT receptor (Ki=3.1 nM) and promotes β-arrestin (EC50=914 nM) and ERK activation (EC50=98 nM) in cells expressing hMT1 receptor. Melatonin-Tamoxifen Conjugate against several common cell lines MCF-7, MDA-MB-231, and HT-1080 with IC50s of 6.8 μM, 6.4 μM, and 1.7 μM, respectively.
