2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor
  4. Clozapine

Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).

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Clozapine Chemical Structure

Clozapine Chemical Structure

CAS No. : 5786-21-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Clozapine:

Clozapine Related Antibodies

Top Publications Citing Use of Products

View All Dopamine Receptor Isoform Specific Products:

View All Isoforms
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

View All mAChR Isoform Specific Products:

View All Isoforms
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

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α adrenergic receptor β adrenergic receptor

View All 5-HT Receptor Isoform Specific Products:

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively[1][2][3]. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[4].

IC50 & Target[1][4]

5-HT2A Receptor

4 nM (Ki, Inhibitor)

5-HT6 Receptor

 

5-HT7 Receptor

 

mAChR1

9.5 nM (Ki, Antagonist)

mAChR4

11 nM (EC50, Agonist)

α2-adrenergic receptor

51 nM (Ki, Inhibitor)

D2 Receptor

75 nM (Ki, Antagonist)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
206 nM
Compound: 1
Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay
Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay
[PMID: 22243698]
CHO IC50
3.6 μM
Compound: clozapine
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 IC50
4.1 x 10-2 μM
Compound: Clozapine
Displacement of [3H]methyl-spiperone from human recombinant dopamine D4.4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]methyl-spiperone from human recombinant dopamine D4.4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO EC50
56 μM
Compound: clozapine
Cytotoxicity against CHO cells by MTT assay
Cytotoxicity against CHO cells by MTT assay
[PMID: 17870534]
HEK293 IC50
650 nM
Compound: Clozapine
Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay
Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay
[PMID: 23675993]
WI-38 EC50
23.26 μM
Compound: Clozapine
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]
WI-38 CC50
40 μM
Compound: Clozapine
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]
In Vitro

Clozapine (HF 1854) is a D2 receptor antagonist with a Ki of 75 nM, blocks the serotonin 5HT2A receptor with a Ki of 4 nM, inhibits the muscarinic M1 receptor with a Ki of 9.5 nM, blocks α2-adrenoceptor with a Ki value of 51 nM[1].
Clozapine (0-1 μM; 24 h) downregulates 5-HT6 and upregulates 5-HT7 receptors in HeLa cells[2].
Clozapine is a full agonist at the muscarinic M4 receptor (EC50=11 nM) expressed in CHO cells[4].

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

Clozapine Related Antibodies
In Vivo

Clozapine (HF 1854) (25 mg/kg/day; i.p.; 21 days) shows antipsychotic effects in lysergic acid diethylamide-induced psychosis mouse model[3].

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

Animal Model: Male 129 S6/Sv mice, lysergic acid diethylamide (LSD)-induced psychosis model[3]
Dosage: 25 mg/kg/day
Administration: Intraperitoneal injection, 21 days
Result: Decreased head-twitch response, reduced 5-HT2A mRNA, rescued induction of c-fos, but not egr-1 and egr-2.
Clinical Trial
Molecular Weight

326.83

Formula

C18H19ClN4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CN1CCN(CC1)C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (152.98 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 3.0597 mL 15.2984 mL 30.5969 mL
5 mM 0.6119 mL 3.0597 mL 6.1194 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (7.65 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 (7.65 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 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:

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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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0597 mL 15.2984 mL 30.5969 mL 76.4921 mL
5 mM 0.6119 mL 3.0597 mL 6.1194 mL 15.2984 mL
10 mM 0.3060 mL 1.5298 mL 3.0597 mL 7.6492 mL
15 mM 0.2040 mL 1.0199 mL 2.0398 mL 5.0995 mL
20 mM 0.1530 mL 0.7649 mL 1.5298 mL 3.8246 mL
25 mM 0.1224 mL 0.6119 mL 1.2239 mL 3.0597 mL
30 mM 0.1020 mL 0.5099 mL 1.0199 mL 2.5497 mL
40 mM 0.0765 mL 0.3825 mL 0.7649 mL 1.9123 mL
50 mM 0.0612 mL 0.3060 mL 0.6119 mL 1.5298 mL
60 mM 0.0510 mL 0.2550 mL 0.5099 mL 1.2749 mL
80 mM 0.0382 mL 0.1912 mL 0.3825 mL 0.9562 mL
100 mM 0.0306 mL 0.1530 mL 0.3060 mL 0.7649 mL
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Clozapine Related Classifications

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:

Clozapine5786-21-0HF 1854HF1854HF-1854Dopamine ReceptormAChRAdrenergic Receptor5-HT ReceptorMuscarinic acetylcholine receptorBeta ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorantipsychoticschizophreniaHeLapsychosisInhibitorinhibitorinhibit

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