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Astemizole

A histamine H1-receptor antagonist and hERG potassium channel blocker
Catalog #: B3050
SKU-Size Size Price Qty
B3050-5 5 mg
$60.00
B3050-25 25 mg
$240.00
More Sizes Get Quote

Product Details

Alternate Name Hismanal; Histaminos; Paralergin; NSC 329963; 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl]benzimidazol-2-amine; 1-(p-Fluorobenzyl)-2-((1-(2-(p-methoxyphenyl)ethyl)piperid-4-yl)amino)benzimidazole; R 43512
Appearance White solid
CAS # 68844-77-9
Molecular Formula C₂₈H₃₁FN₄O
Molecular Weight 458.6
Purity ≥98%
Solubility ~ 5 mg/ml in ethanol, ~10 mg/ml in DMF, ~20 mg/ml in DMSO
SMILES COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
InChi InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31)
InChi Key GXDALQBWZGODGZ-UHFFFAOYSA-N
PubChem CID 2247
MDL Number MFCD00153919
Handling Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Storage Conditions -20ºC
Shipping Conditions RT
USAGE For Research Use Only! Not For Use in Humans.

Details

Astemizole is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG potassium channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole shows synergistic antiproliferative effects with calcitriol in breast cancer cells and in vivo preclinical models by blocking the EAG1 potassium channel. High throughput screens have shown that astemizole is a promising candidate for stopping replication of SARS-CoV-2 virus.


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