Product Data Sheet

Astemizole

Catalog No. A13899

main product photo
Astemizole is a potent antihistamine (H1-receptor antagonist, IC50 = 4 nM) that displays selectivity over dopamine, 5-HT, and muscarinic acetylcholine receptors. This compound has shown potent hERG K+ channel blocking activity (IC50 = 0.9 nM), antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM), and has been used as a chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels.
Adooq's Astemizole has been cited by 1 publications
  • Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
  • Chemical Information
    Catalog Num A13899
    M. Wt 458.57
    Formula C28H31FN4O
    Purity >98%
    Storage at -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
    CAS No. 68844-77-9
    Synonyms Astemisan, Hismanal, Histamen, Paralergim
    SMILES COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
    Storage

    Store lyophilized at -20ºC, keep desiccated.
    In lyophilized form, the chemical is stable for 36 months.
    In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

    Biological Activity
    Discription Astemizole is a potent antihistamine (H1-receptor antagonist, IC50 = 4 nM) that displays selectivity over dopamine, 5-HT, and muscarinic acetylcholine receptors. This compound has shown potent hERG K+ channel blocking activity (IC50 = 0.9 nM), antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM), and has been used as a chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels.
    Solubility
    In vitro DMSO 91 mg/mL (198.44 mM)
    Water Insoluble
    Ethanol 9 mg/mL
    * <1 mg/ml means slightly soluble or insoluble.
    * Please note that Adooq 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.
    Preparing Stock Solutions
    Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
    0.1 mM 21.81 mL 109.03 mL 218.07 mL
    0.5 mM 4.36 mL 21.81 mL 43.61 mL
    1 mM 2.18 mL 10.9 mL 21.81 mL
    5 mM 0.44 mL 2.18 mL 4.36 mL
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    SHIPPING AND STORAGE
    Adooq products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Adooq Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Adooq products are stable under the recommended conditions.