| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Sodium Channel[3]
DPI-201-106 targets voltage-gated sodium channels (VGSCs), specifically the TTX-resistant h1 Na channel. It prolongs the open state of cardiac sodium channels. It also inhibits L-type calcium currents and potassium currents. |
|---|---|
| ln Vitro |
With an EC50 of 0.2 nM, DPI 201-106 raises the Ca2+-sensitivity of peeled fibers from porcine trabecula septomarginalis[2]. Between 0.1 and 3 μM, DPI 201-106 has concentration-dependent positive inotropic effects in the left atria of guinea pigs and rats, as well as in the papillary muscles of kittens, rabbits, and guinea pigs, and in the Langendorff perfused hearts of rabbits[2].
In vitro, DPI-201-106 acts by inhibiting the L-type calcium current, and inward and delayed rectifier potassium currents. This results in a positive inotropic effect. Its activity is assessed in cardiac myocytes by measuring ion channel currents using patch-clamp techniques. |
| ln Vivo |
DPI 201-106 0.2 mg/kg iv increases left ventricular dP/dtmax in dogs under anesthesia. DPI 201-106 is administered up to a cumulative dose of 12.22 mg/kg iv in sedated cats that had received digoxin pretreatment [3].
In vivo, DPI-201-106 has been studied as a cardiotonic agent. Its effects are likely to increase the force of cardiac contraction, which could be beneficial in heart failure. |
| Enzyme Assay |
The assay for sodium channel modulation involves patch-clamp electrophysiology on cells expressing the target sodium channel. Cells are voltage-clamped, and the sodium current is elicited by a depolarizing pulse. Various concentrations of DPI-201-106 are applied, and the inhibition or modulation of the current is measured.
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| Cell Assay |
Cellular assays for DPI-201-106 involve culturing cardiac myocytes or cell lines expressing the target ion channels. The compound's effect on action potential duration and contractility can be measured. Its effects on calcium and potassium currents are assessed using specific electrophysiological protocols.
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| Animal Protocol |
In vivo studies for DPI-201-106 would involve animal models of heart failure. The compound would be administered, and cardiac function would be assessed by measuring parameters such as ejection fraction and cardiac output.
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| ADME/Pharmacokinetics |
DPI-201-106 has a molecular weight of 466.57 g/mol and a molecular formula of C29H30N4O2. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Specific toxicity data for DPI-201-106 is not detailed in the search results. As a cardiotonic agent that modulates ion channels, its therapeutic window is likely narrow.
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| References |
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| Additional Infomation |
4-[3-[4-(diphenylmethyl)-1-piperazinyl]-2-hydroxypropoxy]-1H-indole-2-nitrile is a diarylmethane.
DPI-201-106 is a research compound used to study cardiac ion channels and contractility. It is not an approved drug. Its development may have been discontinued due to safety or efficacy concerns. |
| Molecular Formula |
C29H30N4O2
|
|---|---|
| Molecular Weight |
466.58
|
| Exact Mass |
466.237
|
| Elemental Analysis |
C, 74.65; H, 6.48; N, 12.01; O, 6.86
|
| CAS # |
97730-95-5
|
| Related CAS # |
97730-95-5 (racemic);78573-14-5 (malonate);78573-15-6 (mesylate);161468-21-9 (mesylate 1:1); 97749-21-8 (S-isomer); 97749-20-7 (R-isomer);
|
| PubChem CID |
5190
|
| Appearance |
White to off-white solid powder
|
| Density |
1.29g/cm3
|
| Boiling Point |
702.6ºC at 760mmHg
|
| Flash Point |
378.7ºC
|
| Index of Refraction |
1.692
|
| LogP |
4.062
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
35
|
| Complexity |
672
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N#CC1NC2=CC=CC(OCC(CN3CCN(C(C4=CC=CC=C4)C4=CC=CC=C4)CC3)O)=C2C=1
|
| InChi Key |
BYBYHCOEAFHGJL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C29H30N4O2/c30-19-24-18-26-27(31-24)12-7-13-28(26)35-21-25(34)20-32-14-16-33(17-15-32)29(22-8-3-1-4-9-22)23-10-5-2-6-11-23/h1-13,18,25,29,31,34H,14-17,20-21H2
|
| Chemical Name |
4-[3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropoxy]-1H-indole-2-carbonitrile
|
| Synonyms |
DPI-201-106 (±)-SDZ-201 106 DPI201-106 DPI-201106 DPI 201106 DPI201106 SDZ201 106 SDZ-201106 SDZ 201 106DPI 201-106SDZ 201106 SDZ201106
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~535.83 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.46 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1433 mL | 10.7163 mL | 21.4326 mL | |
| 5 mM | 0.4287 mL | 2.1433 mL | 4.2865 mL | |
| 10 mM | 0.2143 mL | 1.0716 mL | 2.1433 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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