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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
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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 the degree 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 biological activity of the product.
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
If you know of a relevant reference for DPO-1, please let us know.
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Keywords: DPO-1, DPO-1 supplier, blockers, KV15, channel, IKur, current, Potassium, KV, Channels, voltage-gated, voltage-dependent, K+, Diphenylphosphine, oxide1, Diphenyl, phosphine, oxide-1, Voltage-Gated, 2533, Tocris Bioscience
5 Citations for DPO-1
Citations are publications that use Tocris products. Selected citations for DPO-1 include:
Ryland et al (2015) Polycomb-dependent repression of the potassium channel-encoding gene KCNA5 promotes cancer cell survival under conditions of stress. Oncogene 34 4591 PMID: 25435365
Haim et al (2010) Palmitate attenuates myocardial contractility through augmentation of repolarizing Kv currents. J Mol Cell Cardiol 48 395 PMID: 19857498
Zhao et al (2013) Potent suppression of Kv1.3 potassium channel and IL-2 secretion by diphenyl phosphine oxide-1 in human T cells. PLoS One 8 e64629 PMID: 23717641
Ryland et al (2016) Promoter Methylation Analysis Reveals That KCNA5 Ion Channel Silencing Supports Ewing Sarcoma Cell Proliferation. Mol Cancer Res 14 26 PMID: 26573141
Tabarean (2014) Electrical remodeling of preoptic GABAergic neurons involves the Kv1.5 subunit. Pharmacol Res Perspect 9 e96643 PMID: 24797243
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