Astemizole

Name: Astemizole
Brand: Tocris Bioscience
SKU: 3489
Rating: 5 (1 reviews)

Tocris Bioscience a Bio-Techne Brand

Catalog # 3489

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Key Product Details

Description:	Orally active, potent H₁ antagonist; also K_V11.1 (hERG) channel blocker
Alternative Names:	Hismanal
Chemical Name:	1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
Purity:	≥99% (HPLC)
Molecular Weight:	458.57

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Biological Activity for Astemizole

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 K_V11.1 (hERG) channel blocker (IC₅₀ = 0.9 nM) that displays cardiotoxicity in vivo.

Compound Libraries for Astemizole

Astemizole is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Astemizole

M. Wt	458.57
Formula	C₂₈H₃₁FN₄O
Storage	Store at +4°C
Purity	≥99% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Astemizole

	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 will affect the solvent volumes required to prepare stock solutions.

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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References for Astemizole

References are publications that support the biological activity of the product.

Chong A clinical drug library screen identifies astemizole as an antimalarial agent. Nat.Chem.Biol. 2006 PMID: 16816845
Cavalli Towards a pharmacophore for drugs inducing the long QT syndrome: Insights from a CoMFA study of hERG K⁺ channel blockers. J.Med.Chem. 2002 PMID: 12190308
Laduron In vitro and in vivo binding characteristics of a new long-acting histamine H₁ antagonist, astemizole. Mol.Pharmacol. 1981 PMID: 6124876

Citations for Astemizole (1)

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Citations are publications that use Bio-Techne products. Selected citations for Astemizole include:

Klingerman et al. (2014) Second-generation antipsychotics cause a rapid switch to fat oxidation that is required for survival in C57BL/6J mice. Schizophr Bull. 40:327
PMID: 23328157

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Astemizole was used to identify other potential Kv blockers

Name: Anonymous

Species: Human

Assay Type: In Vitro

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.

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