Astemizole

Catalog # Availability Size / Price Qty
3489/50
Astemizole | CAS No. 68844-77-9 | Histamine H1 Receptor Antagonists
1 Image
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

Product Details
Citations (1)
Supplemental Products
Reviews (1)

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.

Technical Data

Formula:
C28H31FN4O
Solubility:
Soluble to 100 mM in DMSO and to 25 mM in ethanol
Storage:
Store the unopened product at 2 - 8 °C. Do not use past expiration date.
CAS No:
68844-77-9

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.

Background References

  1. Towards a pharmacophore for drugs inducing the long QT syndrome: Insights from a CoMFA study of hERG K+ channel blockers.
    Cavalli et al.
    J.Med.Chem., 2002;45:3844
  2. A clinical drug library screen identifies astemizole as an antimalarial agent.
    Chong et al.
    Nat.Chem.Biol., 2006;2:415
  3. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole.
    Laduron et al.
    Mol.Pharmacol., 1981;21:294

Product Datasheets

or select another batch:
Reconstitution Calculator

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Citation for Astemizole

The citations listed below are publications that use Tocris products. Selected citations for Astemizole include:

1 Citation: Showing 1 - 1

FAQs

No product specific FAQs exist for this product, however you may

View all Small Molecule FAQs

Reviews for Astemizole

Average Rating: 5 (Based on 1 Review)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%

Have you used Astemizole?

Submit a review and receive an Amazon gift card.

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Filter by:


Astemizole was used to identify other potential Kv blockers
By Anonymous on 10/31/2018
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.


Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.