
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.
Technical Data
M. Wt | 340.44 |
Formula | C22H29OP |
Storage | Store at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 43077-30-1 |
PubChem ID | 21678144 |
InChI Key | BPCNGVCAHAIZEE-COPCDDAFSA-N |
Smiles | C[C@@H]1CC[C@@H]([C@@H](C)C)[C@@H]([P@@](C2=CC=CC=C2)(C3=CC=CC=C3)=O)C1 |
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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References
References are publications that support the products' biological activity.
Stump et 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
Regan et 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
Lagrutta et 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
Keywords: DPO-1, supplier, blockers, KV15, channel, IKur, current, Potassium, KV, Channels, voltage-gated, voltage-dependent, K+, Diphenylphosphine, oxide1, Diphenyl, phosphine, oxide-1, Voltage-Gated, Potassium, Channels, Voltage-Gated, Potassium, Channels, Tocris Bioscience