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| Targets |
The primary target of DPO-1 is the voltage-gated potassium channel Kv1.5, which underlies the ultrarapid delayed rectifier potassium current (IKur). By blocking Kv1.5 channels, DPO-1 prolongs the atrial action potential duration, which can terminate or prevent atrial arrhythmias. The compound also inhibits Kv1.3 channels (EC50 = 3.1 μM), which are involved in immune cell function. DPO-1 reduces Kv1.3 current density, blunts calcium influx in Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells, indicating potential immunomodulatory and anti-inflammatory effects.
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| ln Vitro |
In vitro, DPO-1 is a potent inhibitor of Kv1.5 channels, which is the basis for its antiarrhythmic activity. It also inhibits Kv1.3 channels with an EC50 of 3.1 μM, demonstrating its potential immunomodulatory effects. In Jurkat cells, DPO-1 reduces Kv1.3 current density, blunts calcium influx in calcium-depleted cells, and inhibits IL-2 secretion in activated cells. The compound is soluble in DMSO at 10 mg/mL (29.37 mM) with ultrasonic warming to 60°C. It is a white to off-white solid and is stored as a powder at -20°C for up to 3 years.
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| ln Vivo |
In vivo, DPO-1 prevents atrial arrhythmia by blocking the Kv1.5 potassium channel and the IKur current. Its ability to selectively target Kv1.5 channels, which are enriched in the atrium, makes it a promising candidate for atrial-selective antiarrhythmic therapy with reduced risk of ventricular proarrhythmia. DPO-1's inhibition of Kv1.3 channels also suggests potential applications in immunomodulation and the treatment of inflammatory diseases. However, detailed in vivo efficacy data in animal models are not extensively reported in the available literature.
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| Enzyme Assay |
In vitro assays for DPO-1 typically involve measuring its inhibition of Kv1.5 or Kv1.3 potassium channels using electrophysiological techniques such as patch-clamp recording in cell lines expressing recombinant channels. The compound is applied to the cells at varying concentrations, and the resulting inhibition of potassium current is measured. The IC50 or EC50 values are determined by fitting concentration-response curves. Radioligand binding assays using [125I]- or [3H]-labeled channel blockers can also be used to assess the compound's affinity for the channel.
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| Cell Assay |
Cellular assays for DPO-1 often utilize Jurkat cells, a human T-cell leukemia cell line, to study its effects on Kv1.3 channels and immune function. Cells are treated with DPO-1 at various concentrations, and Kv1.3 current density is measured using patch-clamp electrophysiology. The compound's effects on calcium influx are assessed using fluorescent calcium indicators, and IL-2 secretion is measured by ELISA. These assays help to characterize the compound's immunomodulatory potential and its mechanism of action on Kv1.3 channels.
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| Animal Protocol |
In vivo animal studies for DPO-1 would typically involve the administration of the compound to animal models of atrial fibrillation or other arrhythmias. The compound could be administered via intravenous injection or oral gavage, and its effects on atrial refractoriness, conduction, and the induction of arrhythmias would be assessed using electrophysiological mapping techniques. In models of inflammation or autoimmune disease, DPO-1 could be administered to study its immunomodulatory effects by measuring inflammatory cytokine levels and immune cell activation. However, specific in vivo study protocols for DPO-1 are not detailed in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for DPO-1 are not extensively reported in the available literature. The compound has a molecular weight of 340.44 g/mol and is soluble in DMSO at 10 mg/mL with warming. It is a white to off-white solid. For research purposes, the compound is typically stored as a powder at -20°C for up to 3 years or in solution at -80°C for up to 6 months. Detailed parameters such as half-life, volume of distribution, and bioavailability are not publicly available and would need to be determined experimentally.
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| Toxicity/Toxicokinetics |
There is no specific toxicity data reported for DPO-1 in the available literature. As a research chemical intended for laboratory use only, it should be handled with standard safety precautions for handling chemical reagents. The compound is not approved for human therapeutic use. Researchers should consult the material safety data sheet (MSDS) for detailed safety and handling information. Any potential toxicity would need to be assessed through formal toxicological studies if the compound were to be developed further.
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| References |
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| Additional Infomation |
[[(1S,2S,5R)-5-methyl-2-propyl-2-ylcyclohexyl]-phenylphosphoyl]benzene is a monoterpene compound.
DPO-1 is a potent inhibitor of the voltage-gated potassium channel subtype Kv1.5 and a blocker of the IKur current. It has a molecular formula of C22H29OP and a molecular weight of 340.44 g/mol. DPO-1 prevents atrial arrhythmia and is a target for novel atrial antiarrhythmic therapy. It also inhibits Kv1.3 channels (EC50 = 3.1 μM), reducing Kv1.3 current and IL-2 secretion. DPO-1 is soluble in DMSO and is stored at -20°C. |
| Molecular Formula |
C22H29OP
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|---|---|
| Molecular Weight |
340.44
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| Exact Mass |
340.196
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| CAS # |
43077-30-1
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| PubChem CID |
21678144
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| Appearance |
White to off-white solid powder
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| Density |
1.054g/cm3
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| Boiling Point |
434.966ºC at 760 mmHg
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| Flash Point |
216.86ºC
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| Index of Refraction |
1.547
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| LogP |
5.461
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
409
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C[C@@H]1CC[C@H]([C@H](C1)P(=O)(C2=CC=CC=C2)C3=CC=CC=C3)C(C)C
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| InChi Key |
BPCNGVCAHAIZEE-COPCDDAFSA-N
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| InChi Code |
InChI=1S/C22H29OP/c1-17(2)21-15-14-18(3)16-22(21)24(23,19-10-6-4-7-11-19)20-12-8-5-9-13-20/h4-13,17-18,21-22H,14-16H2,1-3H3/t18-,21+,22+/m1/s1
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| Chemical Name |
[[(1S,2S,5R)-5-methyl-2-propan-2-ylcyclohexyl]-phenylphosphoryl]benzene
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 10 mg/mL (29.37 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9374 mL | 14.6869 mL | 29.3738 mL | |
| 5 mM | 0.5875 mL | 2.9374 mL | 5.8748 mL | |
| 10 mM | 0.2937 mL | 1.4687 mL | 2.9374 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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