Astemizole

Tocris Bioscience, part of Bio-Techne | Catalog # 3489

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

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.

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

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