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DPO-1

Catalog No. D7443 Name Sigma Aldrich
CAS Number 43077-30-1 Website http://www.sigmaaldrich.com
M. F. C22H29OP Telephone 1-800-521-8956
M. W. 340.438821 Fax
Purity >97% (NMR) Email
Storage protect from light Chembase ID: 153968

SYNONYMS

IUPAC name
{[(1S,2S,5R)-5-methyl-2-(propan-2-yl)cyclohexyl](phenyl)phosphoroso}benzene
IUPAC Traditional name
[(1S,2S,5R)-2-isopropyl-5-methylcyclohexyl(phenyl)phosphoroso]benzene
Synonyms
(1S,2S,5R)-5-Methyl-2-(1-methylethyl)cyclohexyl]diphenyl-phosphine oxide
(+)-Neomenthyl diphenylphosphine oxide

DATABASE IDS

MDL Number MFCD09038567
CAS Number 43077-30-1

PROPERTIES

Empirical Formula (Hill Notation) C22H29OP
Purity >97% (NMR)
Apperance white needles
Solubility DMSO: >5 mg/mL at ~60 °C, clear
MSDS Link Download
Personal Protective Equipment Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter
Storage Condition protect from light
Storage Temperature 2-8°C
German water hazard class 3

DETAILS

Description (English)
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.
Description (简体中文)
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.

REFERENCES