A histamine H1 receptor antagonist (Ki = 4.4 nM) that also blocks ERG potassium channels (IC50 = ~1 nM); used to study long QT syndrome type 2 and as an antineoplastic agent for decreasing proliferation of various cancer cells

Astemizole – 100 mg

Brand:
Cayman
CAS:
68844-77-9
Storage:
-20
UN-No:
Non-Hazardous - /

Astemizole is a non-sedating antihistamine that antagonizes the histamine H1 receptor with a Ki value of 4.4 nM.{25629} It is considerably less potent at muscarinic acetylcholine receptors (Ki = 2.4 µM).{23214} Astemizole is also a potent blocker of ether-a-go-go-related gene (ERG) potassium channels (IC50 = ~1 nM) that has been used to study long QT syndrome type 2.{24505,24504} Furthermore, because it can target oncogenic ERG1 and ERG potassium channels, astemizole has been explored as a potential antineoplastic agent for decreasing proliferation of various cancer cells.{27578}  

 

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Description

A histamine H1 receptor antagonist (Ki = 4.4 nM) that also blocks ERG potassium channels (IC50 = ~1 nM); used to study long QT syndrome type 2 and as an antineoplastic agent for decreasing proliferation of various cancer cells

Formal name: 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine

Synonyms:  NSC 329963

Molecular weight: 458.6

CAS: 68844-77-9

Purity: ≥98%

Formulation: A crystalline solid

Application|Mass Spectrometry||Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Immunology & Inflammation|Allergy

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