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A2861

Astemizole

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

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
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
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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).
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.

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.

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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

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Certificates of Analysis (COA)

Lot/Batch Number
079K4707V
079K47073
079K47072
079K47071
079K4707

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Articles

钾通道

我们可提供多种与钙通道相关的产品以满足您的各类研究需求。

Potassium Channels

We offer many products related to potassium channels for your research needs.

M F Nilsson et al.
Reproductive toxicology (Elmsford, N.Y.), 29(2), 156-163 (2010-02-11)
Drugs blocking the potassium current IKr of the heart (via hERG channel-inhibition) have the potential to cause hypoxia-related teratogenic effects. However, this activity may be missed in conventional teratology studies because repeat dosing may cause resorptions. The aim of the
Chitalu C Musonda et al.
Bioorganic & medicinal chemistry letters, 19(2), 481-484 (2008-12-05)
A dual activity, conjugated approach has been taken to form hybrid molecules of two known antimalarial drugs, chloroquine (CQ) and the non-sedating H1 antagonist astemizole. A variety of linkers were investigated to conjugate the two agents into one molecule. Compounds
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
View All Related Papers

Global Trade Item Number

SKUGTIN
A2861-10MG04061833359822
A2861-50MG04061833359839