Pricing Availability   Qty
Description: Orally active, potent H1 antagonist; also KV11.1 (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)
Citations (1)
Reviews (1)
Literature (1)

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 KV11.1 (hERG) channel blocker (IC50 = 0.9 nM) that displays cardiotoxicity in vivo.

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

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 Data for Astemizole

Solvent Max Conc. mg/mL Max Conc. mM
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.

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 10.9 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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Product Datasheets for Astemizole

Certificate of Analysis / Product Datasheet
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References for Astemizole

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

Cavalli et al (2002) Towards a pharmacophore for drugs inducing the long QT syndrome: Insights from a CoMFA study of hERG K+ channel blockers. J.Med.Chem. 45 3844 PMID: 12190308

Chong et al (2006) A clinical drug library screen identifies astemizole as an antimalarial agent. Nat.Chem.Biol. 2 415 PMID: 16816845

Laduron et al (1981) In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol.Pharmacol. 21 294 PMID: 6124876

If you know of a relevant reference for Astemizole, please let us know.

View Related Products by Product Action

View all Histamine H1 Receptor Antagonists

Keywords: Astemizole, Astemizole supplier, Potent, hERG, K+, channel, blockers, histamine, H1, antagonists, histaminergic, Orally, active, potent, Potassium, KV, Channels, Human, Ether-A-Go-Go, Gene, voltage-gated, voltage-dependent, Receptors, Histamine, KV11.1, Hismanal, Voltage-Gated, 3489, Tocris Bioscience

1 Citation for Astemizole

Citations are publications that use Tocris 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

Do you know of a great paper that uses Astemizole from Tocris? Please let us know.

Reviews for Astemizole

Average Rating: 5 (Based on 1 Review.)

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Astemizole was used to identify other potential Kv blockers.
By Anonymous on 10/31/2018
Assay Type: In Vitro
Species: Human

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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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Histamine Receptors Scientific Review

Histamine Receptors Scientific Review

Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.