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  3. Chlorprothixene

Chlorprothixene is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity.

For research use only. We do not sell to patients.

Chlorprothixene Chemical Structure

Chlorprothixene Chemical Structure

CAS No. : 113-59-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 28 In-stock
Solution
10 mM * 1 mL in DMSO USD 28 In-stock
Solid
50 mg USD 25 In-stock
100 mg USD 40 In-stock
200 mg USD 60 In-stock
500 mg USD 120 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Chlorprothixene:

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Chlorprothixene is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity[1].

IC50 & Target[1]

Human D1 Receptor

18 nM (Ki)

Human D2 Receptor

2.96 nM (Ki)

Human D3 Receptor

4.56 nM (Ki)

Human D5 Receptor

9 nM (Ki)

Human H1 Receptor

3.75 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
77.8 μM
Compound: Chlorprotixen
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
HeLa IC50
1 nM
Compound: chlorprothixene
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
[PMID: 22793499]
In Vitro

Chlorprothixene binds to 5-HT receptors with pKis of 8.3, 8.5, and 9.4 for 5-HT7, 5-HT6 and 5-HT2, respectively[2].

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

Clinical Trial
Molecular Weight

315.86

Formula

C18H18ClNS

CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

CN(C)CC/C=C1C2=C(SC3=C\1C=CC=C3)C=CC(Cl)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (39.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1660 mL 15.8298 mL 31.6596 mL
5 mM 0.6332 mL 3.1660 mL 6.3319 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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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.
Purity & Documentation
References

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 3.1660 mL 15.8298 mL 31.6596 mL 79.1490 mL
5 mM 0.6332 mL 3.1660 mL 6.3319 mL 15.8298 mL
10 mM 0.3166 mL 1.5830 mL 3.1660 mL 7.9149 mL
15 mM 0.2111 mL 1.0553 mL 2.1106 mL 5.2766 mL
20 mM 0.1583 mL 0.7915 mL 1.5830 mL 3.9574 mL
25 mM 0.1266 mL 0.6332 mL 1.2664 mL 3.1660 mL
30 mM 0.1055 mL 0.5277 mL 1.0553 mL 2.6383 mL
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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.

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Product Name:
Chlorprothixene
Cat. No.:
HY-B0274
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