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Clozapine

Cat. No. M3417
Clozapine Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
500mg USD 90 In stock
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Quality Control
Biological Activity

Clozapine (Clozaril) is a potent 5-HT1C receptor antagonist with an IC50 of 110 nM for 5-HT-stimulated phosphoinositide hydrolysis. It is an antipsychotic medication used in the treatment of schizophrenia, and is also used off-label in the treatment of bipolar disorder. Clozapine is classified as an atypical antipsychotic compound because its profile of binding to serotonergic as well as dopamine receptors; its effects on various dopamine mediated behaviors also differ from those exhibited by more typical antipsychotics.

Customer Product Validations & Biological Datas
Source Mol Metab (2017). Figure 2. Clozapine
Method Immunohistochemistry
Cell Lines whole brain
Concentrations 0.3 mg/kg
Incubation Time 0.5 h
Results We found in Figure 2 that hM3Dq-mCherry (in red) was expressed in the brainstem NTS-DMV, and upon ip injection of clozapine-N-oxide (CNO, 0.3 mg/kg), hM3Dq-mediated activation of Gcgþ neurons induced an abundant expression of the early response gene c-Fos (in green, C) in the brainstem NTS-DMV and AP compared to that in A, suggesting activation of Gcgþ neurons-mediated neural circuitry.
Protocol
Cell Experiment
Cell lines A549 and H1299 human NSCLC cells
Preparation method Residual CFSE was then removed by washing twice with phosphate-buffered saline (PBS), followed by cell growth in culture medium with or without 50 μM clozapine for 72 h. For cell cycle analysis, cells were fixed in 70% ethanol and stained with a PI/Triton X-100 DNA-staining solution (20 μg/mL PI, 0.1% Triton X-100, and 0.2 mg/mL RNase A in PBS) at room temperature for 30 min.
Concentrations 50 μM
Incubation time 72 h
Animal Experiment
Animal models specific pathogen–free Sprague-Dawley rats
Formulation water
Dosages 10, 30, and 100 mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 326.82
Formula C18H19ClN4
CAS Number 5786-21-0
Purity 99.99%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

The Drug-Drug Effects of Rhein on the Pharmacokinetics and Pharmacodynamics of Clozapine in Rat Brain Extracellular Fluid by In Vivo Microdialysis.
Hou ML, et al. J Pharmacol Exp Ther. 2015 Oct;355(1):125-34. PMID: 26220937.

Clozapine induces autophagic cell death in non-small cell lung cancer cells.
Yin YC, et al. Cell Physiol Biochem. 2015;35(3):945-56. PMID: 25659606.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Clozapine supplier, 5-HT Receptor, inhibitors

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