Astemizole

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Astemizole is a potent anti-histamine compound that antagonizes the histamine H1-receptor with IC50 of 4 nM. It is also identified less potent at muscarinic acetylcholine receptors with Ki of 2.4 µM. The histamine H1 receptor, a member of Rhodopsin-like G-protein-coupled receptors, is activated by the biogenic amine histamine and is expressed throughout the body, particularly in smooth muscles, on vascular endothelial cells, in the central nervous system, and in the heart. Astemizole targets imperative proteins included in tumor movement, to be specific, either à-go-go 1 (Eag1) and Eag-related quality (Erg) potassium channels. Moreover, Eag1 is thought to be an imperative marker for a few distinct tumors. Astemizole hinders Eag1 and Erg channel action, and in cells communicating the Eag1 channel it diminishes tumor cell expansion in vitro and in vivo. It ought to be noticed that some cardiovascular reactions have been reported for astemizole in a couple of uncommon cases. Nevertheless, astemizole remains as an extremely encouraging hostile to malignancy apparatus on the grounds that it shows anti-proliferative mechanisms, may serve as the basis to synthesize new anti-cancer agents, and has been previously administered clinically. [1]
    
    Reference: 1. Astemizole: an old anti-histamine as a new promising anti-cancer drug. Anticancer Agents Med Chem. 2011 Mar;11(3):307-14.
- Properties
  - Categories
    
    anti-histamine compound, potent
    
    Alternative Name
    
    1-(4-fluorobenzyl)-N-(1-(4-methoxyphenethyl)piperidin-4-yl)-1H-benzo[d]imidazol-2-amine
    
    CAS Number
    
    68844-77-9
    
    Molecular Formula
    
    C28H31FN4O
    
    Molecular Weight
    
    458.57
    
    Appearance
    
    A solid
    
    Purity
    
    99.66%
    
    Solubility
    
    insoluble in H2O; ≥11.46 mg/mL in DMSO with gentle warming; ≥12.46 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    FC1=CC=C(C=C1)CN2C(NC3CCN(CCC(C=C4)=CC=C4OC)CC3)=NC5=CC=CC=C25
    
    * For Research Use Only

Documents

COA (Certificate Of Analysis)

HPLC

NMR (Nuclear Magnetic Resonance)

MSDS (Material Safety Data Sheet)

Datasheet

Astemizole

Background

Documents

We Also Recommend

Cyclosomatostatin

RGDS peptide