Description: Blocker of KV1.5 channel and IKur current
Alternative Names: Diphenyl phosphine oxide-1
Chemical Name: [1S-(1α,2α,5β)]-[5-Methyl-2-(1-methylethyl)cyclohexyl]diphenylphosphine oxide
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Blocker of IKur ultrarapid delayed rectifier potassium current and KV1.5 channels (IC50 = 0.31 μM for rKV1.5). Displays selectivity for inhibition of IKur over Ito (8-fold), IK1, IKr and IKs (20-fold) in native myocytes and selectivity for rat recombinant KV1.5 over KV3.1 (~ 15-fold). Increases action potential duration in atrial but not ventricular myocytes and prevents atrial arrhythmia.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
ethanol
34.04
100
Preparing Stock Solutions
The following data is based on the product molecular weight 340.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.94 mL
14.69 mL
29.37 mL
5 mM
0.59 mL
2.94 mL
5.87 mL
10 mM
0.29 mL
1.47 mL
2.94 mL
50 mM
0.06 mL
0.29 mL
0.59 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Stumpet al (2005) In vivo antiarrhythmic and cardiac electrophysiologic effects of a novel diphenylphosphine oxide IKur blocker (2-isopropyl-5-methylcyclohexyl) diphenylphosphine oxide. J.Pharmacol.Exp.Ther. 315 1362 PMID: 16157659
Reganet al (2006) In vivo cardiac electrophysiologic effects of a novel diphenylphosphine oxide IKur blocker, (2-isopropyl-5-methylcyclohexyl) diphenylphosphine oxide, in rat and nonhuman primate. J.Pharmacol.Exp.Ther. 316 727 PMID: 16243963
Lagruttaet al (2006) Novel, potent inhibitors of human Kv1.5 K+ channels and ultrarapid activating delayed rectifier potassium current. J.Pharmacol.Exp.Ther. 317 1054 PMID: 16522807