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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | $30 | In Stock | In Stock | |
| 25 mg | $42 | In Stock | In Stock | |
| 50 mg | $61 | In Stock | In Stock | |
| 100 mg | $92 | In Stock | In Stock | |
| 500 mg | $302 | Inquiry | Inquiry | |
| 1 mL x 10 mM (in DMSO) | $37 | In Stock | In Stock |

| 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. |
| Synonyms | LX 100-129, HF 1854 |
| Molecular Weight | 326.82 |
| Formula | C18H19ClN4 |
| Cas No. | 5786-21-0 |
| Smiles | CN1CCN(CC1)C1=NC2=C(NC3=C1C=CC=C3)C=CC(Cl)=C2 |
| Relative Density. | 1.31 g/cm3 |
| Storage | In 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
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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