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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $350 | In Stock | |
5 mg | $828 | In Stock | |
10 mg | $1,130 | In Stock | |
25 mg | $1,590 | In Stock | |
50 mg | $1,980 | In Stock | |
100 mg | $2,500 | In Stock | |
500 mg | $4,900 | In Stock |
Description | 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. |
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 |
Smiles | C(CNC(C)=O)C=1C=2C(=CC(Cl)=C(OC)C2)NC1 |
Relative Density. | 1.272g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 90.0 mg/mL (337.4 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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