For research use only.
Catalog No.S2459 Synonyms: HF 1854, LX 100-129
Molecular Weight(MW): 326.82
Clozapine is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.
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Michaelis-Menten plots illustrate the effects of PGD, individual radix paeonia (Pr) and radix glycyrrhiza (Gr) preparations, and the two individual preparations in combination on the formation of N-demethyl-clozapine (A) and clozapine-N-oxide (B) in the human liver microsomes. Serial concentration of clozapine was coincubated in the presence of herbal preparations. The absence of herbal preparations serves as control (CON).
Drug Metab Dispos, 2015, 43(7):1147-53.. Clozapine purchased from Selleck.
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|Description||Clozapine is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.|
Clozapine (10, 20 mg/kg) significantly increases the number of Fos-positive neurons in the nucleus accumbens, medial prefrontal cortex and lateral septal nucleus.  Clozapine induces zif268 but not c-fos mRNA in rat striatum, while Haloperidol induces c-Fos-like immunoreactivity in the caudate-putamen.  Clozapine is more selective for D4 receptors compared to D2 receptors. Clozapine is a mixed but weak D1/D2 antagonist.  Clozapine produces a marked facilitation (300-400%) of NMDA-evoked responses in a concentration-dependent manner with EC50 of 14 nM. Clozapine, but not haloperidol, produces bursts of excitatory postsynaptic potentials (EPSPs), which are blocked by glutamate receptor antagonists, suggesting that these EPSPs are the result of increasing release of excitatory amino acids.  Clozapine is a full agonist at the muscarinic M4 receptor (EC50 = 11 nM), producing inhibition of forskolin-stimulated cAMP accumulation. Clozapine potently antagonizes agonist-induced responses at the other four muscarinic receptor subtypes. 
|In vivo||Clozapine exhibits an "inverted-U" shaped dose-response curve, reversing the apomorphine-induced loss of prepulse inhibition (PPI) at low doses but not at high doses in the rats. Clozapine decreases PPI independent of apomorphine treatment in the rats. |
-  Robertson GS, et al. Neuroscience, 1992, 46(2), 315-328.
-  Nguyen TV, et al. Proc Natl Acad Sci U S A, 1992, 89(10), 4270-4274.
-  Brunello N, et al. Neuropsychopharmacology, 1995, 13(3), 177-213.
|In vitro||DMSO||65 mg/mL (198.88 mM)|
|Ethanol||32 mg/mL (97.91 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||HF 1854, LX 100-129|
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03996356||Not yet recruiting||Other: No study intervention - observational study||Weight Gain|Antipsychotic Agents|Pharmacogenetics||Cwm Taf University Health Board (NHS)||March 2020||--|
|NCT04325386||Active not 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||--|
|NCT03076346||Recruiting||--||Schizophrenia|Treatment-resistant Schizophrenia|Schizoaffective Disorder||University of Pittsburgh||September 1 2017||--|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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