2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. Zuclopenthixol

Zuclopenthixol  (Synonyms: (Z)-Clopenthixol)

製品番号: HY-A0163 純度: 98.08%
COA 取扱説明書 Technical Support

Zuclopenthixol ((Z)-Clopenthixol) is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist.

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Zuclopenthixol

Zuclopenthixol 構造式

CAS 番号 : 53772-83-1

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Based on 1 publication(s) in Google Scholar

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Zuclopenthixol 関連抗体

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製品説明

Zuclopenthixol ((Z)-Clopenthixol) is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist[1][2].

IC50 & Target

D2 Receptor

 

体内実験

After acute treatment, Zuclopenthixol (0.2 and 0.4 mg/kg)-treated animals exhibit ethopharmacological profiles characterized by a decrease in offensive behaviors without impairment of motor activity (0.2 mg/kg). In contrast, the antiaggressive action of the highest dose used (0.4 mg/kg) is accompanied by a marked increase of immobility. After subchronic treatment, no tolerance to Zuclopenthixol antiaggressive or motor activity is observed[1].
Administration of Zuclopenthixol (0.7 and 1.4 mg/kg) significantly elevate MDA level compared to respective controls. Nevertheless, there is no difference between the two dose levels with respect to their effect on rat brain MDA level. Post hoc pairwise comparisons between the means of groups (n=12) receiving different dose levels of Zuclopenthixol reveal that administration of 1.4 mg/kg of Zuclopenthixol significantly reduces GSH level compared to both vehicle-treated and Zuclopenthixol (0.7 mg/kg)-treated animals (P<0.001). Nevertheless, the lower dose of the drug does not affect rat brain GSH level. Animals receiving 0.7 or 1.4 mg/kg of Zuclopenthixol exhibits significantly higher GSH levels than SCO treated animals. Administration of 0.7 mg/kg of Zuclopenthixol significantly elevated GSHPx activity compared to vehicle treated animals[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

400.96

分子式

C22H25ClN2OS
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

OCCN1CCN(CC/C=C2C3=C(SC4=C\2C=CC=C4)C=CC(Cl)=C3)CC1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 200 mg/mL (498.80 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 2.4940 mL 12.4701 mL 24.9401 mL
5 mM 0.4988 mL 2.4940 mL 4.9880 mL
10 mM 0.2494 mL 1.2470 mL 2.4940 mL
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 5 mg/mL (12.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: 2.86 mg/mL (7.13 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.86 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 (28.6 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

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(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).
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
動物実験

Mice[1]
Zuclopenthixol (0.025-0.4 mg/kg) is administered acutely or subchronically for 10 days, on agonistic behavior elicited by isolation in male mice. Individually housed mice are exposed to anosmic "standard opponents" 30 min after the drug administration, and encounters are videotaped and evaluated using an ethologically based analysis[1].
Rats[2]
Male albino rats of Wistar strain weighing 200-250 g are used. They are kept in a temperature of 23-25°C with alternating 12-hour light and dark cycles and allowed free access to food and water. Animals are divided into six groups (n=6). Two groups receive two dose levels of Zuclopenthixol (0.7 and 1.4 mg/kg i.p.) 60 min and SCO (1.4 mg/kg i.p.) 30 min before decapitation. A third group of rats is injected with saline, with the same content of ethanol (20% v/v) and vegetable oil (2.8% v/v) in the test solution, 60 min and then SCO (1.4 mg/kg i.p.) 30 min before decapitation. The forth and fifth groups of rats receive two dose levels of Zuclopenthixol (0.7 and 1.4 mg/kg i.p.) 60 min and saline 30 min before decapitation. A control group of six animals is given saline, with the same content of ethanol (20% v/v) and vegetable oil (2.8% v/v) in the test solution, 60 min and then saline 30 min before decapitation and is run concurrently with drug-treated groups[2].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4940 mL 12.4701 mL 24.9401 mL 62.3504 mL
5 mM 0.4988 mL 2.4940 mL 4.9880 mL 12.4701 mL
10 mM 0.2494 mL 1.2470 mL 2.4940 mL 6.2350 mL
15 mM 0.1663 mL 0.8313 mL 1.6627 mL 4.1567 mL
20 mM 0.1247 mL 0.6235 mL 1.2470 mL 3.1175 mL
25 mM 0.0998 mL 0.4988 mL 0.9976 mL 2.4940 mL
30 mM 0.0831 mL 0.4157 mL 0.8313 mL 2.0783 mL
40 mM 0.0624 mL 0.3118 mL 0.6235 mL 1.5588 mL
50 mM 0.0499 mL 0.2494 mL 0.4988 mL 1.2470 mL
60 mM 0.0416 mL 0.2078 mL 0.4157 mL 1.0392 mL
80 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7794 mL
100 mM 0.0249 mL 0.1247 mL 0.2494 mL 0.6235 mL
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Zuclopenthixol 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:

Zuclopenthixol53772-83-1(Z)-ClopenthixolDopamine ReceptorInhibitorinhibitorinhibit

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