Chlorpromazine

Name: Chlorpromazine
Brand: MedChemExpress
SKU: HY-12708
Rating: 5.0 (58 reviews)

Cat. No.: HY-12708 Purity: 99.61%: FAQs
Data Sheet SDS COA Handling Instructions

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Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT_2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNa_v1.7 channels (IC₅₀=25.9 μM; concentration-dependent) and HERG potassium channels (IC₅₀=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis.

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

Chlorpromazine Chemical Structure

CAS No. : 50-53-3

Size	Price	Stock	Quantity
10 mg	USD 35	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 65	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 98	In-stock	Estimated Time of Arrival: December 31
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Based on 58 publication(s) in Google Scholar

Other Forms of Chlorpromazine:

Chlorpromazine-d₆ hydrochloride In-stock
Chlorpromazine hydrochloride In-stock
Chlorpromazine-d₆ oxalate Get quote

57 Publications Citing Use of MCE Chlorpromazine

: Chlorpromazine purchased from MedChemExpress. Usage Cited in: Commun Biol. 2022 Nov 14;5(1):1248. [Abstract]; Chlorpromazine (CPZ) (10 µM; 30 min) remarkably decreases the cellular internalization of FITC-P-LPK in HCT116 cells. Chlorpromazine can inhibit clathrin-mediated endocytosis. The fluorescence intensity is observed by confocal microscopy and detected using a multi-well plate reader.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

D2 dopamine receptors; 5-HT2A^[1]^[6].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	3.4 μM Compound: chlorpromazine	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
CHO-K1	IC₅₀	1 nM Compound: Chlorpromazine	Antagonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as inhibition of apomorphine-induced calcium mobilization by radiometric and luminescence plate counting method Antagonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as inhibition of apomorphine-induced calcium mobilization by radiometric and luminescence plate counting method	[PMID: 25557493]
CHO-K1	IC₅₀	1 nM Compound: Chlorpromazine	Antagonist activity against human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as reduction in apomorphine-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method Antagonist activity against human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as reduction in apomorphine-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method	[PMID: 25557493]
Cortical neurone	IC₅₀	13.8 μM Compound: Chlorpromazine	Neurotoxicity in rat cortical neuron assessed as inhibition of neurite total length per neuron incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis Neurotoxicity in rat cortical neuron assessed as inhibition of neurite total length per neuron incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis	[PMID: 31841637]
Cortical neurone	IC₅₀	7.99 μM Compound: Chlorpromazine	Neurotoxicity in rat cortical neuron assessed as inhibition of valid neuron count incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis Neurotoxicity in rat cortical neuron assessed as inhibition of valid neuron count incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis	[PMID: 31841637]
Cortical neurone	IC₅₀	9.022 μM Compound: Chlorpromazine	Neurotoxicity in rat cortical neuron assessed as inhibition of neurite outgrowth by measuring mean neurite average length incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis Neurotoxicity in rat cortical neuron assessed as inhibition of neurite outgrowth by measuring mean neurite average length incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis	[PMID: 31841637]
HaCaT	IC₅₀	36.1 μM Compound: CPZ	Phototoxicity in human HaCaT cells assessed as reduction in cell viability preincubated for 60 mins followed by 7.5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay Phototoxicity in human HaCaT cells assessed as reduction in cell viability preincubated for 60 mins followed by 7.5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay	[PMID: 29604584]
HEK293	IC₅₀	27 μM Compound: chlorpromazine	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]
Macrophage cell line	CC₅₀	22.24 μM Compound: CPZ	Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay	[PMID: 28964936]
NCI-H1650	GI₅₀	30.3 μM Compound: Chlorpromazine	Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 26372073]
NHDF	IC₅₀	25.5 μM Compound: CPZ	Phototoxicity in human NHDF cells assessed as reduction in cell viability preincubated for 60 mins followed by 5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay Phototoxicity in human NHDF cells assessed as reduction in cell viability preincubated for 60 mins followed by 5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay	[PMID: 29604584]
Vero	IC₅₀	26.52 μg/mL Compound: CPZ	Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay	[PMID: 32526553]
WI-38	CC₅₀	10.34 μM Compound: Chlorpromazine	Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay	[PMID: 17893158]
WI-38	EC₅₀	7.6 μM Compound: Chlorpromazine	Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay	[PMID: 17893158]

In Vitro

Chlorpromazine (0, 10, 20, 40 μM; 0, 24, 48 h) inhibits growth of U-87MG glioma cells in a dose- and time- dependent manner^[2].
Chlorpromazine (20 μM; 0, 12, 24, 48 h) decreases the levels of cyclin A and cyclin B1 in U-87MG glioma cells, 12 h later^[2].
Chlorpromazine (20 μM) causes inhibition of cell cycle progression^[2].
Chlorpromazine (10 μM; 1 h) significantly suppresses the sEV internalization and dramatically reduces MDSCs in sEV-treated bone marrow cells (MDSCs can significantly suppress the immune cell response, causing immunosuppression in cancer cells)^[3].
Chlorpromazine (3, 10, 20, 40, 60 μM) blocks the hNa_v1.7 current in a concentration-dependent manner^[4].
Chlorpromazine blocks HERG potassium channels with an IC₅₀ value of 21.6 μM and a Hill coefficient of 1.11^[5].

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

Cell Proliferation Assay^[2]

Cell Line:	U-87MG glioma cells
Concentration:	0, 10, 20, 40 μM
Incubation Time:	0, 24, 48 h
Result:	Showed anti-proliferative activity in a dose- and time-dependent manner.

Immunofluorescence^[3]

Cell Line:	Bone marrow cells (sEV-treated)
Concentration:	10 µM
Incubation Time:	1 h
Result:	Reduced MDSCs and suppressed the sEV internalization.

Western Blot Analysis^[2]

Cell Line:	U-87MG glioma cells
Concentration:	20 μM
Incubation Time:	0, 12, 24, 48 h
Result:	Decreased the levels of cyclin A and cyclin B1 12 h later, whereas levels of cyclin D1, proliferating cell nuclear antigen and GAPDH remained unchanged.

In Vivo

Chlorpromazine (20 mg/kg; i.p.; single daily for 7 days) inhibits xenograft tumor growth in nude mouse^[2].

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

Animal Model:	5- to 6-week-old athymic nude mice bearing intracranial U-87MG xenograft tumors^[2].
Dosage:	20 mg/kg
Administration:	Injected intraperitoneally; single daily for 7 days
Result:	Inhibited tumor growth on day 17.

Molecular Weight

318.86

Formula

C₁₇H₁₉ClN₂S

CAS No.

50-53-3

Appearance

Solid

Color

White to off-white

SMILES

CN(C)CCCN1C2=C(C=CC=C2)SC3=CC=C(Cl)C=C13

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (313.62 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	3.1362 mL	15.6809 mL	31.3617 mL
5 mM	0.6272 mL	3.1362 mL	6.2723 mL
10 mM	0.3136 mL	1.5681 mL	3.1362 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (7.84 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% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.84 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 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 (25.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.84 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:

Dosage

mg/kg

Animal weight
(per animal)

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 (protect from light, stored under nitrogen)

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

Purity: 99.61%

Select Batch:

Data Sheet (283 KB) SDS (479 KB)

COA (251 KB) HNMR (164 KB) LCMS (111 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)

References

[1]. Kamgar-Dayhoff P, et al. Multifaceted effect of chlorpromazine in cancer: implications for cancer treatment. Oncotarget. 2021 Jul 6;12(14):1406-1426. [Content Brief]

[2]. Shin SY, et al. The antipsychotic agent chlorpromazine induces autophagic cell death by inhibiting the Akt/mTOR pathway in human U-87MG glioma cells. Carcinogenesis. 2013 Sep;34(9):2080-9. [Content Brief]

[3]. Yang Z, et al. Cancer cell-intrinsic XBP1 drives immunosuppressive reprogramming of intratumoral myeloid cells by promoting cholesterol production. Cell Metab. 2022 Nov 2:S1550-4131(22)00461-2. [Content Brief]

[4]. Lee SJ, et al. Mechanism of inhibition by chlorpromazine of the human pain threshold sodium channel, Nav1.7. Neurosci Lett. 2017 Feb 3;639:1-7. [Content Brief]

[5]. Thomas D, et al. The antipsychotic drug chlorpromazine inhibits HERG potassium channels. Br J Pharmacol. 2003 Jun;139(3):567-74. [Content Brief]

[6]. Suzuki H, et al. Comparison of the anti-dopamine D₂ and anti-serotonin 5-HT(2A) activities of chlorpromazine, bromperidol, haloperidol and second-generation antipsychotics parent compounds and metabolites thereof. J Psychopharmacol. 2013 Apr;27(4):396-400. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.1362 mL	15.6809 mL	31.3617 mL	78.4043 mL
	5 mM	0.6272 mL	3.1362 mL	6.2723 mL	15.6809 mL
	10 mM	0.3136 mL	1.5681 mL	3.1362 mL	7.8404 mL
	15 mM	0.2091 mL	1.0454 mL	2.0908 mL	5.2270 mL
	20 mM	0.1568 mL	0.7840 mL	1.5681 mL	3.9202 mL
	25 mM	0.1254 mL	0.6272 mL	1.2545 mL	3.1362 mL
	30 mM	0.1045 mL	0.5227 mL	1.0454 mL	2.6135 mL
	40 mM	0.0784 mL	0.3920 mL	0.7840 mL	1.9601 mL
	50 mM	0.0627 mL	0.3136 mL	0.6272 mL	1.5681 mL
	60 mM	0.0523 mL	0.2613 mL	0.5227 mL	1.3067 mL
	80 mM	0.0392 mL	0.1960 mL	0.3920 mL	0.9801 mL
	100 mM	0.0314 mL	0.1568 mL	0.3136 mL	0.7840 mL

Chlorpromazine Related Classifications

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Chlorpromazine

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57 Publications Citing Use of MCE Chlorpromazine

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Chlorpromazine

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Chlorpromazine Related Antibodies

57 Publications Citing Use of MCE Chlorpromazine

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