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D7443 Sigma

DPO-1

needles, >97% (NMR)

Synonym: (+)-Neomenthyl diphenylphosphine oxide, (1S,2S,5R)-5-Methyl-2-(1-methylethyl)cyclohexyl]diphenyl-phosphine oxide

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, DIG-DY,
InChI Key   BPCNGVCAHAIZEE-COPCDDAFSA-N
assay   >97% (NMR)
form   needles
storage condition   protect from light
color   white
solubility   DMSO: 2 mg/mL clear (warmed)
storage temp.   2-8°C

Description

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

DPO-1 is an inhibitor of human Kv1.5 potassium channel; representative blocker of a novel pharmacophore. The Kv1.5 potassium channel, which underlies the ultrarapid delayed rectifier current, IKur, is reported to be enriched in human atrium versus ventricle, and has been proposed as a target for novel atrial antiarrhythmic therapy. The administration of the IKur blocker (2-isopropyl-5-methyl-cyclohexyl) diphenylphosphine oxide (DPO-1) increases myocardial refractoriness in both atrium and ventricle of rat, but produces an atrial-selective increase in refractoriness in primates; appears to be 15-fold more selective for Kv1.5 vs Kv3.1 channels expressed in Xenopus oocytes. IC50 = 0.16-0.76 μM at 0.1 Hz pulsing frequency; Kd = 0.6 μM.

Features and Benefits

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

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.

Legal Information

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Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
3

Documents

Certificate of Analysis

Protocols & Articles

Articles

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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