Chlorprothixene

Alias: MK 184; N 714; N 714C; NSC 1872;0 Paxyl; Rentovet; Ro 4-0403; N-714;MK-184;Taractan; Tarasan; Chlorprothixene

Cat No.:V1259 Purity: ≥98%

COA Product Data Instructions for use SDS

Chlorprothixene Chemical Structure CAS No.: 113-59-7
Product category: Dopamine Receptor

This product is for research use only, not for human use. We do not sell to patients.

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1g
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Other Forms of Chlorprothixene:

Chlorprothixene HCl

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

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Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information

Product Description

Chlorprothixene (Paxyl; Rentovet; Truxal; Ro 4-0403; N-714; MK-184; Taractan; Tarasan), an typical antipsychotic drug of the thioxanthene class, is an antagonist of dopamine and histamine receptors with potential antipsychotic, sedative and antiemetic activity. It inhibits the following dopamine receptors: D1, D2, D3, D5, histamine receptors H1, 5-HT2, and serotonin receptors 5-HT6/7 with Ki values of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.

Biological Activity I Assay Protocols (From Reference)

Targets

Human D₁ Receptor ( Ki = 18 nM ); Human D₂ Receptor ( Ki = 2.96 nM ); Human D₃ Receptor ( Ki = 4.56 nM ); Human D₅ Receptor ( Ki = 9 nM ); Human H₁ Receptor ( Ki = 3.75 nM )

ln Vitro

In vitro activity: Chlorprothixene has little affinity for H3, but it exhibits strong binding affinities to dopamine and histamine receptors, such as D1, D2, D3, D5, and H1, with Ki values of 18 nM, 2.96 nM, 4.56 nM, 9 nM, and 3.75 nM, respectively.[1] Furthermore, rat 5-HT6 from stably transfected HEK-293 cells and rat 5-HT7 receptors from transiently expressed COS-7 cells exhibit strong affinities for chlorprothixene, with Ki values of 3 nM and 5.6 nM, respectively.[2] Chlorprothixene administration inhibits the replication of SARS-CoV in Vero 76 cells, with IC50 values of 16.7 μM for the Urbani strain, 13.0 μM for Frankfurt-1, 18.5 μM for CHUK-W1, and 15.8 μM for Toronto-2. They resemble those found using promazine.[3]

ln Vivo

Chlorprothixene suppresses the release of hypothalamic and hypophyseal hormones by blocking postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain. Chlorprothixene at high doses prevents iproniazid from protecting the adrenal medulla and brain from the catecholamines released by reserpine, as well as from decreasing the amounts of 5HT, NE, and DA in the rat brain as a result of reserpine or iproniazid.[4] By inhibiting acidsphingomyelinase (Asm) rather than neutral sphingomyelinase (Nsm), chlorprothixene administration restores normal ceramide concentrations in murine bronchial epithelial cells, reduces inflammation in the lungs of mice with cystic fibrosis (CF), and prevents infection with Pseudomonas aeruginosa.[5]

Animal Protocol

Dissolved in 0.9% NaCl solution, final concentration 8 mg/L; 1 mL every time; Five 10-minute inhalations, every 12 hours

B6.129P2 (CF/3)-CftrTgH(neoim)Hgu (abbreviated CFMHH) congenic mice.

References

[1]. Bioorg Med Chem Lett . 2009 Jan 15;19(2):538-42.

[2]. J Pharmacol Exp Ther . 1994 Mar;268(3):1403-10.

[3]. Antiviral Res . 2008 Aug;79(2):105-13.

[4]. J Pharmacol Exp Ther . 1961 Jul:133:18-24.

[5]. Am J Respir Cell Mol Biol . 2010 Jun;42(6):716-24.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C18H18CLNS

Molecular Weight

315.86

Exact Mass

315.08

Elemental Analysis

C, 68.45; H, 5.74; Cl, 11.22; N, 4.43; S, 10.15

CAS #

113-59-7

Related CAS #

Chlorprothixene hydrochloride; 6469-93-8

Appearance

Solid powder

SMILES

CN(C)CC/C=C\1/C2=CC=CC=C2SC3=C1C=C(C=C3)Cl

InChi Key

WSPOMRSOLSGNFJ-AUWJEWJLSA-N

InChi Code

InChI=1S/C18H18ClNS/c1-20(2)11-5-7-14-15-6-3-4-8-17(15)21-18-10-9-13(19)12-16(14)18/h3-4,6-10,12H,5,11H2,1-2H3/b14-7-

Chemical Name

(3Z)-3-(2-chlorothioxanthen-9-ylidene)-N,N-dimethylpropan-1-amine;hydrochloride

Synonyms

MK 184; N 714; N 714C; NSC 1872;0 Paxyl; Rentovet; Ro 4-0403; N-714;MK-184;Taractan; Tarasan; Chlorprothixene

HS Tariff Code

2934.99.03.00

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 6~33.3 mg/mL (19~105.5 mM)

Water: <1 mg/mL

Ethanol: ~28 mg/mL (~88.6 mM)

Preparing Stock Solutions		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
	10 mM	0.3166 mL	1.5830 mL	3.1660 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03449485	Recruiting	Drug: Chlorprothixene	Obesity, Morbid	Norwegian University of Science and Technology	January 2, 2018	N/A