2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Buclizine dihydrochloride

Buclizine dihydrochloride  (Synonyms: ブクリジン, 二塩酸塩)

製品番号: HY-A0128A 純度: 99.62%
COA 取扱説明書 Technical Support

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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Buclizine dihydrochloride

Buclizine dihydrochloride 構造式

CAS 番号 : 129-74-8

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Buclizine dihydrochloride 関連抗体

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製品説明

Buclizine dihydrochloride is an orally active antihistamine antiallergic compound. Buclizine dihydrochloride is a potent teratogen in the rat and shows anti-tumor activity[1][2][3].

体外実験

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.

Buclizine dihydrochloride 関連抗体

Cell Proliferation Assay[2].

Cell Line: MCF-7 cells[3].
Concentration: 0-100 μM.
Incubation Time: 72 hours
Result: Showed considerable growth inhibition (IC50=19.18 μM).

Western Blot Analysis[2].

Cell Line: MCF-7 cells
Concentration: 0-75 μM
Incubation Time: 72 hours
Result: Decreased TCTP expression by 40% at 75 μM.
Decreased cyclin D1, cyclin D3, CDK2 and CDK4 expression after 72 h.
体内実験

Buclizine dihydrochloride (30-200 mg/kg; tenth to fifteenth and twelfth to fifteenth days of gestation) shows potent teratogens in the rat[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eighty-seven mature female rats weighing 240±20 grams[3].
Dosage: 30, 40, 60, 100, and 200 mg/kg
Administration: 30-200 mg/kg; tenth to fifteenth and twelfth to fifteenth days of gestation
Result: Resulted in malformations in 100% of the young at a dose level of 60-100 mg/kg.
分子量

505.95

分子式

C28H35Cl3N2
CAS 番号
Appearance

Solid

Color

White to off-white

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9765 mL 9.8824 mL 19.7648 mL
5 mM --- --- ---
10 mM --- --- ---
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション
参考文献

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
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Buclizine dihydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Buclizine129-74-8Histamine Receptorantihistamineantiallergicanti-tumor activityteratogenMCF-7Inhibitorinhibitorinhibit

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製品名:
Buclizine dihydrochloride
製品番号:
HY-A0128A
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