Astemizole

Tocris Bioscience | Catalog # 3489

Orally active, potent H1 antagonist; also KV11.1 (hERG) channel blocker
Tocris Bioscience

Key Product Details

Description

Orally active, potent H1 antagonist; also KV11.1 (hERG) channel blocker

Alternative Names

Hismanal
View all Histamine H1 Receptor Antagonists »

Product Description

Astemizole is an orally active, potent histamine H1 antagonist (IC50 = 4 nM) that displays 20-fold, > 250-fold and > 250-fold selectivity over 5-HT, dopamine and muscarinic acetylcholine receptors respectively. Exhibits antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM). Also potent KV11.1 (hERG) channel blocker (IC50 = 0.9 nM) that displays cardiotoxicity in vivo.

Product Specifications for Astemizole

Molecular Weight

458.57

Formula

C28H31FN4O

Storage

Store at +4°C

Purity

≥98% (HPLC)

Chemical Name

1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine

CAS Number

68844-77-9

PubChem ID

2247

InChI Key

GXDALQBWZGODGZ-UHFFFAOYSA-N

SMILES

FC(C=C5)=CC=C5CN2C1=CC=CC=C1N=C2NC3CCN(CCC4=CC=C(OC)C=C4)CC3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.86 100
Ethanol 11.46 25

Preparing Stock Solutions for Astemizole

The following data is based on the product molecular weight 458.57.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.18 mL 10.90 mL 21.81 mL
5 mM 0.44 mL 2.18 mL 4.36 mL
10 mM 0.22 mL 1.09 mL 2.18 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 13 publications citing the usage of this product.

Product Documents for Astemizole

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for Astemizole

For research use only

Customer Reviews for Astemizole (1)

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  • Astemizole was used to identify other potential Kv blockers
    Name: Anonymous
    Species: Human
    Assay Type: In Vitro
    Verified Customer | Posted 10/31/2018
    Astemizole is a great well known histaminic drug which shows Kv channel blocking at high concentrations. It was used on our lab to identify other potential Kv blockers. While using it as a standard, it worked ideally all during the study period.
    Astemizole 3489

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