Clozapine (HF 1854)

Alias: HF-1854; LX 100-129; HF 1854; LX 100129; HF1854; LX100129; Leponex; Fazaclo; CLOZARIL; Clozapin; Clozaril
Cat No.:V0962 Purity: ≥98%
Clozapine(LX 100129; HF1854, LX100129; Leponex; Fazaclo; CLOZARIL; Clozapin; Clozaril) is an atypical antipsychotic drug wand a 5-HT antagonist used in the treatment of schizophrenia.
Clozapine (HF 1854) Chemical Structure CAS No.: 5786-21-0
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
5g
10g
Other Sizes

Other Forms of Clozapine (HF 1854):

  • Clozapine-d8
  • Clozapine-d4
  • Clozapine N-oxide
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Clozapine (LX 100129; HF1854, LX100129; Leponex; Fazaclo; CLOZARIL; Clozapin; Clozaril) is an atypical antipsychotic drug wand a 5-HT antagonist used in the treatment of schizophrenia. It binds to receptors for dopamine and serotonin. With its partial agonistic action at the 5-HT1A subunit of the serotonin receptor, clozapine may help alleviate symptoms of anxiety, depression, and negative cognitive symptoms linked to schizophrenia. There has also been evidence of clozapine's direct interaction with the GABAB receptor. Mice lacking the GABAB receptor show altered locomotor behavior and elevated extracellular dopamine levels similar to animal models of schizophrenia.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT2A Receptor ( Ki = 4 nM ); 5-HT6 Receptor; 5-HT7 Receptor; mAChR1 ( Ki = 9.5 nM ); mAChR4 ( Ki = 11 nM ); α2-adrenergic receptor ( Ki = 51 nM ); D2 Receptor ( Ki = 75 nM )
ln Vitro

In vitro activity: Clozapine (10, 20 mg/kg) enhances the quantity of Fos-positive neurons in the lateral septal nucleus, medial prefrontal cortex, and nucleus accumbens considerably. In rat striatum, clozapine induces zif268 but not c-fos mRNA. In the caudate-putamen, haloperidol induces c-Fos-like immunoreactivity.[2] Clozapine prefers D4 receptors over D2 receptors in terms of selectivity. Clozapine functions as a weak, mixed D1/D2 antagonist.[3] Clozapine ignificantly facilitates (300–400%) NMDA-evoked responses in a concentration-dependent manner with EC50 of 14 nM. Excitatory postsynaptic potentials (EPSPs) are triggered by clozapine but not by haloperidol. These EPSPs are inhibited by glutamate receptor antagonists, indicating that the increased release of excitatory amino acids is the cause of these EPSPs.[4] With an EC50 of 11 nM, clozapine is a full agonist at the muscarinic M4 receptor, inhibiting the accumulation of cAMP stimulated by forskolin. Across the other four muscarinic receptor subtypes, clozapine potently opposes the effects of agonist-induced responses.[5]

ln Vivo
Clozapine shows a dose-response curve with a "inverted-U" shape, reversing the rats' loss of prepulse inhibition (PPI) caused by apomorphine at low doses but not at high ones. In rats treated with apomorphine or not, clozapine reduces PPI.[6]
Animal Protocol
25 mg/kg
Mice: Mice are treated chronically (21 days) with 25 mg/kg/day clozapine. Experiments are conducted 1, 7, 14, and 21 days after the last clozapine administration. [3H]Ketanserin binding and 5-HT2A mRNA expression are determined in mouse somatosensory cortex. Head-twitch behavior, expression of c-fos, which is induced by all 5-HT2A agonists, and expression of egr-1 and egr-2, which are LSD-like specific, are assayed
References

[1]. Neuroscience . 1992;46(2):315-28.

[2]. Proc Natl Acad Sci U S A . 1992 May 15;89(10):4270-4.

[3]. Neuropsychopharmacology . 1995 Nov;13(3):177-213.

[4]. J Pharmacol Exp Ther . 1997 Oct;283(1):226-34.

[5]. Eur J Pharmacol . 1994 Nov 15;269(3):R1-2.

[6]. J Pharmacol Exp Ther . 1991 Feb;256(2):530-6.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H19CLN4
Molecular Weight
326.82
Exact Mass
326.13
Elemental Analysis
C, 66.15; H, 5.86; Cl, 10.85; N, 17.14
CAS #
5786-21-0
Appearance
Solid powder
SMILES
CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)NC4=CC=CC=C42
InChi Key
QZUDBNBUXVUHMW-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3
Chemical Name
3-chloro-6-(4-methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepine
Synonyms
HF-1854; LX 100-129; HF 1854; LX 100129; HF1854; LX100129; Leponex; Fazaclo; CLOZARIL; Clozapin; Clozaril
HS Tariff Code
2934.99.9001
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: 50~65 mg/mL (153~198.9 mM)
Water: <1 mg/mL
Ethanol: ~32 mg/mL (~97.9 mM)
Solubility (In Vivo)
5%DMSO + Corn oil: 5.0mg/ml (15.30mM) (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0598 mL 15.2989 mL 30.5979 mL
5 mM 0.6120 mL 3.0598 mL 6.1196 mL
10 mM 0.3060 mL 1.5299 mL 3.0598 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

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g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.

(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.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02714894 Active
Recruiting
Drug: Clozapine Schizophrenia Centre for Addiction and
Mental Health
April 2016 N/A
NCT04325386 Active
Recruiting
Other: Education Sessions
Other: No Education Session
Schizophrenia Schizoaffective University of Maryland, Baltimore February 1, 2020 Not Applicable
NCT04074213 Recruiting Drug: Clozapine Lymphoma
Leukemia
University Hospital, Caen March 1, 2019 N/A
NCT05208190 Recruiting Drug: Clozapine
Drug: treatment as usual
Schizophrenia
Schizoaffective Disorder
New York State Psychiatric
Institute
March 17, 2022 Phase 4
NCT05316883 Recruiting Drug: Clozapine Schizophrenia
Psychosis
Mental Health Services in the
Capital Region, Denmark
February 28, 2021 Phase 4
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