Astemizole

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Cat.No. 3489 - Astemizole | C28H31FN4O | CAS No. 68844-77-9
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)
Datasheet
Citations (1)
Literature

Biological Activity

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.

Compound Libraries

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

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 458.57. Batch specific molecular weights may vary from batch to batch due to solvent 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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:


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View Related Products by Product Action

View all Histamine H1 Receptor Antagonists

Keywords: 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 Histamine H1 Receptors

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


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Literature in this Area

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Pathways for Astemizole

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