6-Chloromelatonin
Based on 1 Customer Validation
6-Chloromelatonin is a potent melatonin receptor agonist with greater metabolic stability than melatonin. 6-Chloromelatonin compete for [3H]-melatonin and 2-[125I]-iodomelatonin binding to MT1 receptors (pKi=8.9 and 9.1, respectively). 6-Chloromelatonin compete for [3H]-melatonin binding to MT2 receptors (pKi=9.77).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.50%
- No. CAS: 63762-74-3
- Fòrmula: C13H15ClN2O2
- Peso molecular:266.72
-
Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
HY-101254
LuzindoleMelatonin Receptor Antagonist -
HY-100609
4-P-PDOTMT2 Receptor Antagonist -
HY-101176
2-IodomelatoninMT1 Agonist -
HY-101358
8-M-PDOTMT2 Receptor Agonist -
HY-14803
TasimelteonDual Melatonin Receptor Agonist -
HY-A0014
RamelteonMT1/2 Inhibitor -
HY-101074
UCM 608Melatonin Agonist -
HY-101254R
Luzindole (Standard)Melatonin Receptor Antagonist -
HY-100609R
4-P-PDOT (Standard)MT2 Receptor Antagonist -
HY-100908
N-AcetyltryptamineMelatonin Receptor Mixed Agonist-Antagonist -
HY-107628
N-Pentanoyl 2-benzyltryptamineMT2 Antagonist -
HY-101176R
2-Iodomelatonin (Standard)MT1 Agonist
Actividad biológica
Descripciòn
IC50 & Target
[1]|
MT1 8.9 (pKi) |
MT2 9.1 (pKi) |
In Vitro
6-Chloromelatonin competes for [3H]-melatonin binding sites in human platelet (Ki=11.4 nM)[3].
6-chloromelatonin (10 pM, 1 nM, 100 nM, 10 μM; 72 hours) inhibits, in a dose-dependent manner, forskolin-stimulated hCG-beta secretion in JEG-3 and BeWo cells but had no effect on basal human chorionic gonadotrophin (hCG-beta) levels[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 63762-74-3
-
Appearance Solid
-
Peso molecular 266.72
-
Fòrmula C13H15ClN2O2
-
Color White to off-white
-
SMILES
CC(NCCC1=CNC2=C1C=C(OC)C(Cl)=C2)=O
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (374.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (275 KB)
-
SDS (421 KB)
- English - EN (421 KB)
- Français - FR (421 KB)
- Deutsch - DE (421 KB)
- Norwegian - NO (421 KB)
- Español - ES (421 KB)
- Swedish - SV (421 KB)
- Italian - IT (421 KB)
- Korean - KR (421 KB)
- Portuguese - PT (421 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[2]. Clemens JA, et al. Inhibition of luteinizing hormone release and ovulation by 6-chloro- and 6-fluoromelatonin. Neuroendocrinology. 1980;30(2):83-87. [Content Brief]
[3]. Vacas MI, et al. Binding sites for [3H]-melatonin in human platelets. J Pineal Res. 1992;13(2):60-65. [Content Brief]
[4]. Lanoix D, et al. Expression of melatoninergic receptors in human placental choriocarcinoma cell lines. Hum Reprod. 2006;21(8):1981-1989. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7493 mL | 18.7463 mL | 37.4925 mL | 93.7313 mL |
| 5 mM | 0.7499 mL | 3.7493 mL | 7.4985 mL | 18.7463 mL | |
| 10 mM | 0.3749 mL | 1.8746 mL | 3.7493 mL | 9.3731 mL | |
| 15 mM | 0.2500 mL | 1.2498 mL | 2.4995 mL | 6.2488 mL | |
| 20 mM | 0.1875 mL | 0.9373 mL | 1.8746 mL | 4.6866 mL | |
| 25 mM | 0.1500 mL | 0.7499 mL | 1.4997 mL | 3.7493 mL | |
| 30 mM | 0.1250 mL | 0.6249 mL | 1.2498 mL | 3.1244 mL | |
| 40 mM | 0.0937 mL | 0.4687 mL | 0.9373 mL | 2.3433 mL | |
| 50 mM | 0.0750 mL | 0.3749 mL | 0.7499 mL | 1.8746 mL | |
| 60 mM | 0.0625 mL | 0.3124 mL | 0.6249 mL | 1.5622 mL | |
| 80 mM | 0.0469 mL | 0.2343 mL | 0.4687 mL | 1.1716 mL | |
| 100 mM | 0.0375 mL | 0.1875 mL | 0.3749 mL | 0.9373 mL |
6-Chloromelatonin Related Classifications
HY-100940 Related Classifications
Powered by Bioz