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6-Chloromelatonin

Catalog No. T22530 CAS 63762-74-3

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

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6-Chloromelatonin, CAS 63762-74-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 350.00
5 mg	In stock	$ 828.00
10 mg	In stock	$ 1,130.00
25 mg	In stock	$ 1,590.00
50 mg	In stock	$ 1,980.00
100 mg	In stock	$ 2,500.00
500 mg	In stock	$ 4,900.00

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Purity: 99.36%

Purity: 98.01%

Purity: 97.90%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	6-Chloromelatonin is a potent melatonin receptor agonist, a 5-methoxyindole compound that competes for the same presynaptic melatonin receptor sites in the rabbit retina and inhibits the calcium-dependent release of [3H]dopamine with a higher metabolic stability than melatonin. Chloromelatonin competes for [3H]melatonin binding to MT2 receptors (pKi=9.77) and may be used to study insomnia and sleep disorders associated with depression.
Targets&IC50	MT2:9.1 (pKi), MT1:8.9 (pKi)
In vitro	6-Chloromelatonin (10 pM, 1 nM, 100 nM, 10 μM; 72 h) inhibits forskolin-stimulated hCG-beta secretion in JEG-3 and BeWo cells in a dose-dependent manner but had no effect on basal human chorionic gonadotrophin (hCG-beta) levels.[4] 6-Chloromelatonin competes for [3H]-melatonin binding sites in human platelet (Ki=11.4 nM).[3]
In vivo	6-Chloromelatonin (0.5 mg/kg; injection; rats) on the day after the phase shift has markedly higher excretion rates of 6-Sulphatoxymelatonin compared with controls.[5]

Molecular Weight	266.72
Formula	C13H15ClN2O2
CAS No.	63762-74-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (337.4 mM), Sonication is recommended.

References and Literature

1. Browning C, et al. Pharmacological characterization of human recombinant melatonin mt(1) and MT(2) receptors. Br J Pharmacol. 2000;129(5):877-886. 2. Clemens JA, et al. Inhibition of luteinizing hormone release and ovulation by 6-chloro- and 6-fluoromelatonin. Neuroendocrinology. 1980;30(2):83-87. 3. Vacas MI, et al. Binding sites for [3H]-melatonin in human platelets. J Pineal Res. 1992;13(2):60-65. 4. Lanoix D, et al. Expression of melatoninergic receptors in human placental choriocarcinoma cell lines. Hum Reprod. 2006;21(8):1981-1989. 5. Kennaway DJ, et al. A melatonin agonist and N-acetyl-N2-formyl-5-methoxykynurenamine accelerate the reentrainment of the melatonin rhythm following a phase advance of the light-dark cycle. Brain Res. 1989;495(2):349-354.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library GPCR Compound Library Bioactive Compound Library Neurotransmitter Receptor Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library

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Related compounds with same targets

Tasimelteon Melatonin Ramelteon Luzindole 4-P-PDOT ACH-000143 N-ACETYLTRYPTAMINE Agomelatine

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Keywords

6-Chloromelatonin 63762-74-3 GPCR/G Protein Neuroscience Dopamine Receptor Melatonin Receptor 6 Chloromelatonin 6Chloromelatonin inhibitor inhibit

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