Cycleanine
Based on 1 Customer Validation
Cycleanine is a potent vascular selective Calcium antagonist. Cycleanine has analgesic, muscle relaxant and anti-inflammatory activities. Cycleanine has potential for anti-ovarian cancer acting through the apoptosis pathway.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.80%
- No. CAS: 518-94-5
- Fòrmula: C38H42N2O6
- Peso molecular:622.75
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
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L-type calcium channel |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
7.6 μM
Compound: 1
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Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay
Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay
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[PMID: 29588214] |
| IGROV-1 | IC50 |
14 μM
Compound: 1
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Antiproliferative activity against human IGROV1 cells after 72 hrs by SRB assay
Antiproliferative activity against human IGROV1 cells after 72 hrs by SRB assay
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[PMID: 29588214] |
| OVCAR-8 | IC50 |
10 μM
Compound: 1
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Antiproliferative activity against human OVCAR8 cells after 72 hrs by SRB assay
Antiproliferative activity against human OVCAR8 cells after 72 hrs by SRB assay
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[PMID: 29588214] |
In Vitro
Cycleanine inhibits L-type Ca-current (ICaL) of single rat ventricular cardiomyocytes in a voltage- and frequency-dependent manner[1].
Cycleanine shows modestly less potency against human OSE cells (normal) than the cancer cells[2].
Cycleanine (20 μM; 48 hours) exhibits cytotoxicity for Ovcar-8, A2780, Igrov-1, and Ovcar-4 cell lines with IC50s ranging from 7 to 14 μM[2].
Cycleanine (20 μM; 24 hours) results in significant PARP cleavage (a marker of apoptosis)[2].
Cycleanine (20 μM; 48 hours) causes a significant increase of the population of both early and late apoptotic cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ovcar-8 cells, A2780 cells, Igrov-1 cells, Ovcar-4 cells
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Concentration:20 μM
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Incubation Time:48 hours
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Result:Exhibited cytotoxicity for Ovcar-8, A2780, Igrov-1, and Ovcar-4 cell lines with IC50 values of 10 μM, 7.6 μM, 14 μM, 7.2 μM, respectively.
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Cell Line:Ovcar-8 cells
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Concentration:20 μM
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Incubation Time:24 hours
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Result:Induced 1.1-fold increase in PARP-1 cleavage compared with carboplatin.
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Cell Line:Ovcar-8 cells
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Concentration:20 μM
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Incubation Time:48 hours
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Result:Caused a significant increase of the population of both early and late apoptotic cells.
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Cell Line:Ovcar-8 cells
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Concentration:20 μM
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Incubation Time:48 hours
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Result:Increased the percentage of Ovcar-8 cells in subG1.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 518-94-5
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Appearance Solid
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Peso molecular 622.75
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Fòrmula C38H42N2O6
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Color White to off-white
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SMILES
COC1=C(OC2=CC=C(C[C@](N(CC3)C)([H])C4=C3C=C5OC)C=C2)C([C@@](N6C)([H])CC7=CC=C(OC4=C5OC)C=C7)=C(CC6)C=C1OC
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
In Vitro:
DMSO : 5 mg/mL (8.03 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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: 0.5 mg/mL (0.80 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 0.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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: 0.5 mg/mL (0.80 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
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Ficha de datos (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Martínez JA, et al. Calcium antagonist properties of the bisbenzylisoquinoline alkaloid cycleanine. Fundam Clin Pharmacol. 1998;12(2):182-7. [Content Brief]
[2]. Uche FI, et al. Cytotoxicity Effects and Apoptosis Induction by Bisbenzylisoquinoline Alkaloids from Triclisia subcordata. Phytother Res. 2016 Sep;30(9):1533-9. [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 (sealed storage, away from moisture and light). 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 | 1.6058 mL | 8.0289 mL | 16.0578 mL | 40.1445 mL |
| 5 mM | 0.3212 mL | 1.6058 mL | 3.2116 mL | 8.0289 mL |
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