Skip to Content
Merck

Key Documents

View All Documentation

A2861

Astemizole

≥98% (HPLC), hERG potassium channel blocker, powder

Synonym(s):

1-(4-Fluorobenzyl)-2-(1-[4-methoxyphenethyl]piperidin-4-yl)aminobenzimidazole

Sign In to View Organizational & Contract Pricing.

Select a Size

Change View

About This Item

Empirical Formula (Hill Notation):
C28H31FN4O
CAS Number:
68844-77-9
Molecular Weight:
458.57
NACRES:
NA.77
PubChem Substance ID:
329770802
UNSPSC Code:
41121800
EC Number:
272-441-9
MDL number:
MFCD00153919
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
desiccated, protect from light
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist

Product Name

Astemizole, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated, protect from light

solubility

DMSO: >20 mg/mL

originator

Johnson & Johnson

storage temp.

2-8°C

SMILES string

COc1ccc(CCN2CCC(CC2)Nc3nc4ccccc4n3Cc5ccc(F)cc5)cc1

InChI

1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31)

InChI key

GXDALQBWZGODGZ-UHFFFAOYSA-N

Gene Information

human ... HRH1(3269)

Biochem/physiol Actions

Astermizole is a potent hERG potassium channel blocker (IC50 of 0.9 nM) and may used as a pharmacological chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels. It has also been studied for treatment of malaria, hERG and hEAG channel function in cancer and as a second generation antihistamine H-1 antagonist.
Astermizole is a potent hERG potassium channel blocker (IC50 of 0.9 nM).

Features and Benefits

This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Still not finding the right product?

Explore all of our products under Astemizole

pictograms

Exclamation mark
GHS07

signalword

Warning

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

target_organs

Respiratory system

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Choose from one of the most recent versions:

Certificates of Analysis (COA)

Lot/Batch Number
0000512177
0000512177
0000499943
0000499943
0000451522

Don't see the Right Version?

If you require a particular version, you can look up a specific certificate by the Lot or Batch number.

Search for a COA

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Fumimasa Nomura et al.
Journal of nanobiotechnology, 9, 39-39 (2011-09-21)
Conventional in vitro approach using human ether-a-go-go related gene (hERG) assay has been considered worldwide as the first screening assay for cardiac repolarization safety. However, it does not always oredict the potential QT prolongation risk or pro-arrhythmic risk correctly. For
K A Rao et al.
Mayo Clinic proceedings, 69(6), 589-593 (1994-06-01)
An overdose of astemizole predisposes the myocardium to ventricular dysrhythmias, including torsades de pointes. Herein we describe a case of astemizole-induced torsades de pointes ventricular tachycardia and also review previous case reports in the literature. All the patients were young
Kiem Vu et al.
Medical mycology, 48(2), 255-262 (2009-07-03)
Cryptococcus neoformans is the leading cause of fungal meningitis, a life-threatening infection that occurs predominately in immuocompromised patients. Current drug therapies are limited to amphotericin B, flucytosine and the azoles since the echinocandins have no demonstrated activity against yeast like
View All Related Papers