Art. -Nr.: HY-14539A

Clozapine hydrochloride

(Synonyms: HF 1854 hydrochloride)

11 Cited Publications

Kundenbewertung

Based on 11 publication(s) in Google Scholar

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

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Reinheit: 99.83%
CAS. Nr.: 54241-01-9
Formel: C₁₈H₂₀Cl₂N₄
Molecular Weight:363.28

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Clozapine hydrochloride Chemical Structure

CAS. Nr.: 54241-01-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

5-HT_2A Receptor

4 nM (Ki)

5-HT_2A Receptor

5-HT₆ Receptor

Human 5-HT₇ Receptor

mAChR1

9.5 nM (Ki)

mAChR4

11 nM (EC₅₀)

α2-adrenergic receptor

51 nM (Ki)

D₂ Receptor

75 nM (Ki)

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

Alle mAChR Isoform-spezifische Produkte anzeigen :

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

In Vivo

Clozapine hydrochloride (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-HT_2A mRNA, rescued induction of c-fos, but not egr-1 and egr-2.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 54241-01-9
Appearance Solid
Molecular Weight 363.28
Formel C₁₈H₂₀Cl₂N₄
Color Light yellow to yellow
SMILES

CN1CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42)CC1.[H]Cl
Synonyms

HF 1854 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (11)

All Cell Imaging/StainingBio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

Nat Commun

Norepinephrine-mediated arousal fluctuations drive inverted U-shaped functional connectivity dynamics. [Abstract]

2025 Dec 13;16(1):11318. PMID: 41390822

Clozapine hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Dec 13;16(1):11318. [Abstract]

In isoflurane anesthetized mice, the injection of Clozapine (0.03 mg/kg; i.p.) significantly increased EEG-based arousal index, but from a low to middle arousal level.
Nat Commun

Feedforward inhibition of stress by brainstem neuropeptide Y neurons. [Abstract]

2024 Sep 1;15(1):7603. PMID: 39217143

Clozapine hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 1;15(1):7603. [Abstract]

Representative current clamp recording of a NPY^DRN/vlPAG-hM4Di neuron with the bath of Clozapine (5 μM). Average membrane potential and firing frequency before and after Clozapine application to inhibit NPY ^DRN/vlPAGneurons were also recorded. Clozapine effectively inhibited hM4Di⁺ NPY^DRN/vlPAG neurons with decreased neuronal membrane potential and firing frequency.

Clozapine hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 1;15(1):7603. [Abstract]

Percentage of body weight changes, daily food intake and its area under curve (AUC) of mCherry-restraint and hM4Di-restraint mice. Clozapine (i.p.; 0.2mg/kg; 30 min before restraint for 14 d) caused NPY^hM4Di mice to consume less food and lost more body weight than NPY^mCherry mice during chronic restraint stress.
Mol Psychiatry

ZFP804A mutant mice display sex-dependent schizophrenia-like behaviors. [Abstract]

2021 Jun;26(6):2514-2532. PMID: 33303946

Clozapine hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Psychiatry. 2021 Jun;26(6):2514-2532. [Abstract]

The administration of Clozapine (i.p.; 2 d) restored impaired PPI in female ZFP804A mutant mice.
Commun Med (Lond)

AI-enabled drug prediction and gene network analysis reveal therapeutic use of vorinostat for Rett Syndrome in preclinical models. [Abstract]

2025 Jul 1;5(1):249. PMID: 40595330
Eur J Pharm Sci

Investigating the relevance of CYP2J2 inhibition for drugs known to cause intermediate to high risk torsades de pointes. [Abstract]

2023 Aug 1:187:106475. PMID: 37225005
Eur J Pharm Sci

Atypical kinetics of cytochrome P450 2J2: Epoxidation of arachidonic acid and reversible inhibition by xenobiotic inhibitors. [Abstract]

2021 Sep 1:164:105889. PMID: 34044117
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
FEBS J

TRPM7 controls skin keratinocyte senescence by targeting intracellular calcium signaling. [Abstract]

2024 Nov;291(21):4680-4695. PMID: 39185948

Clozapine hydrochloride purchased from MedChemExpress. Usage Cited in: FEBS J. 2024 Nov;291(21):4680-4695. [Abstract]

HaCaT cells were transfected with siNC or siRNA against TRPM7 and then treated with Clozapine (Clo) (10 μM; 6 d) the next day. Clozapine (Clo) promoted activation of TRPM7 and increased SA-b-Gal activity.
Biochem Biophys Res Commun

Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]

2025 Oct 30:786:152756. PMID: 41043280
bioRxiv

2024 November 03.
bioRxiv

Functional coupling between MC4R and Kir7.1 contributes to clozapine-induced hyperphagia. [Abstract]

2024 Jun 8:2024.06.07.597973. PMID: 38895206

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (275.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7527 mL

13.7635 mL

27.5270 mL

5 mM

0.5505 mL

2.7527 mL

5.5054 mL

10 mM

0.2753 mL

1.3763 mL

2.7527 mL

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

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (6.88 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.88 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.88 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Seeman P, et al. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9. [Content Brief]

[2]. Zhukovskaya NL, et al. Clozapine downregulates 5-hydroxytryptamine6 (5-HT6) and upregulates 5-HT7 receptors in HeLa cells. Neurosci Lett. 2000 Jul 21;288(3):236-40. [Content Brief]

[3]. Moreno JL, et al. Persistent effects of chronic clozapine on the cellular and behavioral responses to LSD in mice. Psychopharmacology (Berl). 2013 Jan;225(1):217-26. [Content Brief]

[4]. Zorn SH, et al. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269(3):R1-2. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7527 mL	13.7635 mL	27.5270 mL	68.8174 mL
	5 mM	0.5505 mL	2.7527 mL	5.5054 mL	13.7635 mL
	10 mM	0.2753 mL	1.3763 mL	2.7527 mL	6.8817 mL
	15 mM	0.1835 mL	0.9176 mL	1.8351 mL	4.5878 mL
	20 mM	0.1376 mL	0.6882 mL	1.3763 mL	3.4409 mL
	25 mM	0.1101 mL	0.5505 mL	1.1011 mL	2.7527 mL
	30 mM	0.0918 mL	0.4588 mL	0.9176 mL	2.2939 mL
	40 mM	0.0688 mL	0.3441 mL	0.6882 mL	1.7204 mL
	50 mM	0.0551 mL	0.2753 mL	0.5505 mL	1.3763 mL
	60 mM	0.0459 mL	0.2294 mL	0.4588 mL	1.1470 mL
	80 mM	0.0344 mL	0.1720 mL	0.3441 mL	0.8602 mL
	100 mM	0.0275 mL	0.1376 mL	0.2753 mL	0.6882 mL

Keywords

Clozapine hydrochloride

11 Cited Publications

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Clozapine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Clozapine hydrochloride

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Alle mAChR Isoform-spezifische Produkte anzeigen

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Clozapine hydrochloride Related Classifications

Art. -Nr.: HY-14539A