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Astemizole

Name: Astemizole
Brand: SIGMA

≥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

Storage condition:

desiccated, protect from light

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Properties

Product Name

Astemizole, ≥98% (HPLC)

Quality Segment

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)

Description

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.

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This Item	SML0851	A8106	SML2940
Sigma-Aldrich A2861 Astemizole	Sigma-Aldrich SML0851 GZ-793A	Sigma-Aldrich A8106 Altanserin hydrochloride hydrate	Sigma-Aldrich SML2940 ML417
description ≥98% (HPLC)	description ≥98% (HPLC)	description ≥98% (HPLC), solid	description ≥98% (HPLC)
form powder	form powder	form solid	form powder
assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C
solubility DMSO: >20 mg/mL	solubility H₂O: 3 mg/mL, clear	solubility DMSO: >5 mg/mL, H₂O: insoluble	solubility DMSO: 2 mg/mL, clear
storage condition protect from light, desiccated	storage condition -	storage condition -	storage condition -

Pictograms

GHS07

Signal Word

Warning

Hazard Codes

H315,H319,H335

Precautionary Statements

P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338

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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