A derivative of fluphenazine that contains an alkylating chlorethylamine chain

Fluphenazine-N-2-chloroethane (hydrochloride) – 50 mg

Brand:
Cayman
CAS:
3892-78-2
Storage:
-20
UN-No:
Non-Hazardous - /

Fluphenazine is a traditional antipsychotic compound that tightly binds the dopamine D2 receptor (Ki = 0.55 nM) and also reversibly inhibits calmodulin at micromolar concentrations.{26444,30053} Fluphenazine-N-2-chloroethane is a derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding.{30056,30051} It is a relatively selective, irreversible antagonist of D2 receptors both in vitro (IC50 = 100 nM) and in vivo, inactivating approximately 90% of D2 receptors in mice within 4 hours of treatment.{30054,30055} Through this action, fluphenazine-B-2-chloroethane can be used to induce catalepsy in mice.{30054,30050} It irreversibly inhibits calmodulin at higher doses (IC50 = 10 µM), which can sensitize cancer cells to TRAIL-induced apoptosis.{30056,30052}  

 

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Description

A derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding; a relatively selective, irreversible antagonist of D2 receptors both in vitro (IC50 = 100 nM) and in vivo; irreversibly inhibits calmodulin at higher doses (IC50 = 10 µM)

Formal name: 10-[3-[4-(2-chloroethyl)-1-piperazinyl]propyl]-2-(trifluoromethyl)-10H-phenothiazine dihydrochloride

Synonyms:  Fluphenazine-N-mustard|FNM|FPCE|SKF-7171A

Molecular weight: 528.9

CAS: 3892-78-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|DNA Alkylating Agents||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis

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