melatonin

Melatonin (Melatonine) is a natural hormone secreted by the pineal gland that activates melatonin receptors. Melatonin is a hormone that regulates the biological clock and also has antioxidant and anti-inflammatory activities.

2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, exhibiting over 5-fold selectivity for MT1 compared to MT2. It can be used to identify, characterize, and localize melatonin binding sites in the brain and peripheral tissues.

6-Chloromelatonin is a potent melatonin receptor agonist, a 5-methoxyindole compound that competes for presynaptic melatonin receptor sites in the rabbit retina, inhibiting the calcium-dependent release of [3H]dopamine with higher metabolic stability than melatonin. Chloromelatonin competitively binds to [3H]melatonin at MT2 receptors (pKi=9.77) and may be used to study insomnia and sleep disorders associated with depression.

Melatonin D5, a deuterium-labeled version of melatonin, is a hormone produced by the pineal gland, known for its role as a selective ATF-6 inhibitor that promotes apoptosis in human hepatoma cells via COX-2 downregulation. Additionally, it activates melatonin receptors and exhibits antioxidative and anti-inflammatory properties.

4-P-PDOT (4-phenyl-2- propionamidotetralin) is a potent, selective and affinity Melatonin receptor (MT2) antagonist.

Agomelatine (Valdoxan) is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors, tested in an animal model of depression.

Ramelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.

Luzindole (N-0774) is a selective melatonin receptor antagonist that inhibits experimental autoimmune encephalomyelitis and exhibits antidepressant-like activity. It preferentially targets MT2 (Mel1b) over MT1 (Mel1a), with Ki values of 10.2 nM for human MT2 and 158 nM for MT1.

S26131 (N-[2-[7-[3-[8-(2-acetamidoethyl)naphthalen-2-yl]oxypropoxy]naphthalen-1-yl]ethyl]acetamide) behaves as an antagonist on MT1 and MT2 receptors with Ki of 0.5 and 112 nM respectively.

TIK-301 is a chlorinated melatonin derivative and a potent, high-affinity, and orally active melatonin MT1 and MT2 receptors agonist (Kis: 0.081 nM and 0.042 nM, respectively). TIK-301 is also a 5-HT2B/5-HT2C receptor antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.

Tasimelteon (BMS-214778) is a melatonin receptor agonist that is used for the treatment of non-24 hour sleep-wake disorder in blind individuals.

N-ACETYLTRYPTAMINE is a partial agonist for melatonin receptors in the retina. Also used for determination of serotonin N-acetyl transferase.

ACH-000143 have been identified as a novel agonist of the melatonin receptors MT1 and MT2.

Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate made of Melatonin and Tamoxifen, serving as an effective antagonist of ERα (IC50 = 863 nM). In cells expressing the hMT1 receptor, it binds to MLT receptors (Ki = 3.1 nM) and exhibits the ability to promote β-arrestin activation (EC50 = 914 nM) and ERK activation (EC50 = 98 nM). The IC50 values for Melatonin-Tamoxifen Conjugate in MCF-7, MDA-MB-231, and HT-1080 cell lines are 6.8 μM, 6.4 μM, and 1.7 μM, respectively.

Melatonin receptor agonist 1 (compound 20c) is a potent agonist of the melatonin receptor (MT) with Ki values of 108 nM for MT2 and 1140 nM for MT1 [1].

Melatonin Biotin is a useful organic compound for research related to life sciences and the catalog number is T64745.

Melatonin (Standard) is a reference material for melatonin, suitable for quantitative analysis, quality control, and biochemical research. Melatonine is a naturally occurring hormone secreted by the pineal gland that activates melatonin receptors and regulates the circadian rhythm, exhibiting antioxidant and anti-inflammatory activities.

6-Hydroxymelatonin is the main active metabolite and endogenous metabolite of Melatonin via CYP1A2, an agonist of MT2 receptor with antioxidant and neuroprotective effects, and effectively reduces KCN-induced lipid peroxidation and superoxide anion production.

MELATONIN(ACETYL-d3) is a deuterated compound of MELATONIN. MELATONIN has a CAS number of 73-31-4. Melatonin is a biogenic amine that is found in animals and plants. In mammals, melatonin is produced by the PINEAL GLAND. Its secretion increases in darkness and decreases during exposure to light. Melatonin is implicated in the regulation of SLEEP, mood, and REPRODUCTION. Melatonin is also an effective antioxidant.

6-Sulfatoxy Melatonin-d4 is a deuterated compound of 6-Sulfatoxy Melatonin. 6-Sulfatoxy Melatonin has a CAS number of 2208-40-4.

Agomelatine hydrochloride (S-20098 hydrochloride) is a specific MT1 and MT2 receptor agonist with Ki values of 0.1 nM for CHO-hMT1, 0.06 nM for HEK-hMT1, 0.12 nM for CHO-hMT2, and 0.27 nM for HEK-hMT2, respectively [1]. Additionally, Agomelatine hydrochloride is a selective antagonist of the 5-HT2C receptor with pKi values of 6.4 and 6.2 for native (porcine) and cloned human 5-HT2C receptors, respectively [2].

N-Acetyl-5-hydroxytryptamine (O-Demethylmelatonin) , also known as Normelatonin, is the immediate precursor of melatonin. It is produced from serotonin by the enzyme aralkylamine N-acetyltransferase and is converted to melatonin by acetylserotonin O-methyltransferase. It can potently activate TrkB receptor.

8-M-PDOT (AH-002) is a selective and potent melatonin MT2 receptor agonist that also inhibits MT1 receptors. 8-M-PDOT exhibits anxiolytic activity and can be used to study MT2-induced neuropathic pain.

Ramelteon metabolite M-II is the primary metabolite of Ramelteon and exhibits IC50 values of 208 pM and 1470 pM for human melatonin receptors (MT1 and MT2), respectively. Ramelteon itself is a selective melatonin receptor agonist.