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Clozapine

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Catalog No. T0455Cas No. 5786-21-0
Alias LX 100-129, HF 1854

Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

Clozapine

Clozapine

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Purity: 99.93%
Catalog No. T0455Alias LX 100-129, HF 1854Cas No. 5786-21-0
Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$30In StockIn Stock
25 mg$42In StockIn Stock
50 mg$61In StockIn Stock
100 mg$92In StockIn Stock
500 mg$302InquiryInquiry
1 mL x 10 mM (in DMSO)$37In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.93%
Color:White to Yellow
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Product Introduction

Clozapine AI Summary
Clozapine exhibits a wide range of pharmacological activities across various receptor systems and demonstrates significant potential for therapeutic implications. It shows high affinity for serotonin 5-hydroxytryptamine receptors 2A (Ki = 3.68 nM) and 2C (Ki = 10.47 nM), as well as dopamine receptors, particularly D4 (Ki = 10.0 nM) and D2 (Ki = 223.87 nM). The compound displays strong binding to adrenergic alpha-1 receptors (Ki = 1.4 nM) and muscarinic acetylcholine receptors (IC50 = 12.0 nM). It inhibits multiple behaviors induced by apomorphine and DOI in rodent models, with effective doses ranging from 2.2 mg/kg to approximately 26.2 mg/kg. Clozapine shows moderate liver distribution (Vdss = 5.4 L/kg), low unbound fraction in plasma (Fu = 0.05), and significant metabolic stability. Additionally, it also affects the heart by inhibiting the human ERG channel (IC50 = 323.59 nM). Despite its wide receptor interactions, including histamine H1 and various dopamine and serotonin receptors, its potential therapeutic application in conditions related to adrenergic, dopaminergic, and serotonergic signaling, and its detailed pharmacokinetic profile make it a compound of considerable interest for further investigation..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.
Targets&IC50
M4 mAChR:11 nM (EC50, agonist), α2-adrenoceptor:51 nM (Ki, inhibitor), M1 mAChR:9.5 nM(Ki), D2 Receptor:75 nM (Ki, antagonist), 5-HT2A receptor:4 nM (Ki, inhibitor)
In vitro
Clozapine significantly facilitated NMDA-evoked responses in a concentration-dependent manner (EC50: 14 nM).Clozapine produced excitatory postsynaptic potentials, which were blocked by glutamate receptor antagonists, suggesting that these excitatory postsynaptic potentials were the result of an increased release of excitatory amino acids.Clozapine is a full agonist at muscarinic M4 receptors, with an EC50=11 nM, and a -logEC50=6.52.The EC50=11 nM. Clozapine is a full agonist at muscarinic M4 receptors, with an EC50=11 nM, and inhibits forskolin-stimulated cAMP accumulation.Clozapine is a potent antagonist of agonist-induced responses at four other muscarinic receptor subtypes.
In vivo
Clozapine significantly facilitated NMDA-evoked responses in a concentration-dependent manner (EC50: 14 nM).Clozapine produced excitatory postsynaptic potentials, which were blocked by glutamate receptor antagonists, suggesting that these excitatory postsynaptic potentials were the result of an increased release of excitatory amino acids.Clozapine is a full agonist at muscarinic M4 receptors, with an EC50=11 nM, and a -logEC50=6.52.The EC50=11 nM. Clozapine is a full agonist at muscarinic M4 receptors, with an EC50=11 nM, and inhibits forskolin-stimulated cAMP accumulation.Clozapine is a potent antagonist of agonist-induced responses at four other muscarinic receptor subtypes.
SynonymsLX 100-129, HF 1854
Chemical Properties
Molecular Weight326.82
FormulaC18H19ClN4
Cas No.5786-21-0
SmilesCN1CCN(CC1)C1=NC2=C(NC3=C1C=CC=C3)C=CC(Cl)=C2
Relative Density.1.31 g/cm3
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 82.5 mg/mL (252.43 mM), Sonication is recommended.
2eq.HCl: 16.3 mg/mL (49.87 mM), Heating is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.12 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
2eq.HCl/DMSO
1mg5mg10mg50mg
1 mM3.0598 mL15.2989 mL30.5979 mL152.9894 mL
5 mM0.6120 mL3.0598 mL6.1196 mL30.5979 mL
10 mM0.3060 mL1.5299 mL3.0598 mL15.2989 mL
20 mM0.1530 mL0.7649 mL1.5299 mL7.6495 mL
DMSO
1mg5mg10mg50mg
50 mM0.0612 mL0.3060 mL0.6120 mL3.0598 mL
100 mM0.0306 mL0.1530 mL0.3060 mL1.5299 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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