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A6424

Sigma-Aldrich

Astemizole

≥99%

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C28H31FN4O
CAS Number:
68844-77-9
Molecular Weight:
458.57
EC Number:
272-441-9
MDL number:
MFCD00153919
UNSPSC Code:
12352100
PubChem Substance ID:
24891087

Assay

≥99%

SMILES string

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

Gene Information

human ... ABCB1(5243) , CYP3A4(1576) , HRH1(3269) , IL4(3565) , IL5(3567) , KCNH1(3756) , KCNH2(3757)
mouse ... Abcb1a(18671) , Abcb1b(18669)
rat ... Hrh1(24448)

Biochem/physiol Actions

Non-sedating anti-histaminergic drug. Substrate for CYP3A4,5,7. Inhibitor of Pgp-mediated drug efflux and Pgp labeling by [3H]azidopine. Potential for combination therapy with anticancer drugs such as doxorubicin in resistant leukemia.

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H315,H319,H335

Precautionary Statements

P261 - P305 + P351 + P338

Hazard Classifications

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

Storage Class Code

13 - Non Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

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Certificates of Analysis (COA)

Lot/Batch Number
087K1207
040K1522
113K0704
065H0195
083H0928

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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
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
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
Anida Hasanovic et al.
Biomedicines, 8(8) (2020-08-06)
Adrenocortical carcinoma (ACC) presents a high risk of relapse and metastases with outcomes not improving despite extensive research and new targeted therapies. We recently showed that the Hedgehog receptor Patched is expressed in ACC, where it strongly contributes to doxorubicin
Andrew M Sawayama et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 15(43), 11723-11729 (2009-09-24)
Herein we demonstrate that a small panel of variants of cytochrome P450 BM3 from Bacillus megaterium covers the breadth of reactivity of human P450s by producing 12 of 13 mammalian metabolites for two marketed drugs, verapamil and astemizole, and one
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