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A2861 Sigma

Astemizole

≥98% (HPLC)

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

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Properties

Related Categories AN-AZ, Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology,
InChI Key   GXDALQBWZGODGZ-UHFFFAOYSA-N
assay   ≥98% (HPLC)
form   powder
storage condition   desiccated
  protect from light
solubility   DMSO: >20 mg/mL
originator   Johnson & Johnson
storage temp.   2-8°C

Description

Packaging

10, 50 mg in glass bottle

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.

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.

Other Notes

Tandem Mass Spectrometry data independently generated by Scripps Center for Metabolomics is available to view or download in PDF. A2861.pdf Tested metabolites are featured on Scripps Center for Metabolomics METLIN Metabolite Database. To learn more, visit sigma.com/metlin.

Safety & Documentation

Safety Information

Symbol 
GHS07  GHS07
Signal word 
Warning
Hazard statements 
Precautionary statements 
RIDADR 
NONH for all modes of transport
WGK Germany 
3
RTECS 
DD8968000

Documents

Certificate of Analysis


Discover your Target

Making Headway
Protocols & Articles

Articles

Discover Bioactive Small Molecules for Ion Channels Research

Ion transport across the relatively impermeable lipid bilayer of the cell membrane is accomplished via membrane proteins known as ion channels, pumps and transporters. Ion channels are gated pores an...
Keywords: Biological processes, Cell signaling, Diseases, Hormones, Ligands, Neurotransmitters

Potassium Channels

Potassium channels are essential in both excitable and non-excitable cells for the control of membrane potential, regulation of cell volume, and the secretion of salt, neurotransmitters and hormones....
Keywords: Absorption, Cancer, Cell proliferation, Cell signaling, Diabetes, Diseases, Hormones, Ligands, Neurotransmitters, Phosphorylations, Sequencing

Peer-Reviewed Papers
15

References

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