Buclizine dihydrochloride
Based on 1 Customer Validation
Buclizine dihydrochloride is an orally active antihistamine antiallergic compound. Buclizine dihydrochloride is a potent teratogen in the rat and shows anti-tumor activity.
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- Pureza: 99.62%
- No. CAS: 129-74-8
- Fòrmula: C28H35Cl3N2
- Peso molecular:505.95
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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- Referencias
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Actividad biológica
Buclizine (0.1-100 μM; 72 h) inhibits growth of MCF-7 cells[2].
Buclizine (9.625-77 μM; 72 h) arrests the cell cycle in the G1 phase in a dose-dependent manner[2].
Buclizine (0-75 μM; 72 h) decreases TCTP (translationally controlled tumor protein) and cell cycle regulatory proteins expression in MCF-7 cells, increases pro-apoptotic MCL-1S expression[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells[3].
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Concentration:0-100 μM.
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Incubation Time:72 hours
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Result:Showed considerable growth inhibition (IC50=19.18 μM).
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Cell Line:MCF-7 cells
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Concentration:9.625, 19.25, 38.5, and 77 μM
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Incubation Time:72 hours
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Result:Increased the percentages of cells in the G1 phase to 73% at 77 μM.
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Cell Line:MCF-7 cells
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Concentration:0-75 μM
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Incubation Time:72 hours
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Result:Decreased TCTP expression by 40% at 75 μM.
Decreased cyclin D1, cyclin D3, CDK2 and CDK4 expression after 72 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eighty-seven mature female rats weighing 240±20 grams[3].
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Dosage:30, 40, 60, 100, and 200 mg/kg
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Administration:30-200 mg/kg; tenth to fifteenth and twelfth to fifteenth days of gestation
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Result:Resulted in malformations in 100% of the young at a dose level of 60-100 mg/kg.
Chemical Information
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No. CAS 129-74-8
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Appearance Solid
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Peso molecular 505.95
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Fòrmula C28H35Cl3N2
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Color White to off-white
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SMILES
CC(C1=CC=C(CN2CCN(C(C3=CC=C(Cl)C=C3)C4=CC=CC=C4)CC2)C=C1)(C)C.[H]Cl.[H]Cl
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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
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 2.5 mg/mL (4.94 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 (sealed storage, away from moisture). 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). 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)
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 (0.99 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
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 (0.99 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
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.
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)
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 (274 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Gamal A E Mostafa, et al. Buclizine. Profiles Drug Subst Excip Relat Methodol. 2011;36:1-33. [Content Brief]
[2]. C T King, et al. Teratogenic effect of buclizine and hydroxyzine in the rat and chlorcyclizine in the mouse. Am J Obstet Gynecol. 1966 May 1;95(1):109-11. [Content Brief]
[3]. Ean-Jeong Seo, et al. Interaction of antihistaminic drugs with human translationally controlled tumor protein (TCTP) as novel approach for differentiation therapy. Oncotarget. 2016 Mar 29;7(13):16818-39. [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). 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 | 1.9765 mL | 9.8824 mL | 19.7648 mL | 49.4120 mL |
Buclizine dihydrochloride Related Classifications
HY-A0128A Related Classifications
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