Astemizole | B3050

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.

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.

B3050 | Astemizole DataSheet

Alternate Name/Synonyms: 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

Formulation:

CAS Number: 68844-77-9

Structure Available?: TRUE

Peptide sequence:

Salt Form: FALSE

Molecular Formula: C₂₈H₃₁FN₄O

Molecular Weight: 458.6

Cell-Permeable?: TRUE

Purity: ≥98%

Solubilities: ~ 5 mg/ml in ethanol, ~10 mg/ml in DMF, ~20 mg/ml in DMSO

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A histamine H1-receptor antagonist and hERG potassium channel blocker

MDL Number: MFCD00153919

PubChem CID: 2247

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