| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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DPI-201-106 [(±)-SDZ-201 106] is a novel and potent inhibitor of the TTX-resistant h1 Na channel which is cardioselective. It acts by inhibiting the L-type calcium current, and inward and delayed rectifier potassium currents. As a cardiotonic agent, it has a synergistic sarcolemmal and intracellular mechanism of action.
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| 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].
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| 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].
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| References |
[1]. G Scholtysik, et al. DPI 201-106, a novel cardioactive agent. Combination of cAMP-independent positive inotropic, negative chronotropic, action potential prolonging and coronary dilatory properties. Naunyn Schmiedebergs Arch Pharmacol.1985 May;329(3):316-
[2]. G Scholtysik, et al. Interaction of DPI 201-106 with cardiac glycosides. J Cardiovasc Pharmacol. 1989 Feb;13(2):342-7. [3]. M Mevissen, et al. Identification of a cardiac sodium channel insensitive to synthetic modulators. J Cardiovasc Pharmacol Ther. 2001 Apr;6(2):201-12. |
| Molecular Formula |
C29H30N4O2
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|---|---|
| Molecular Weight |
466.58
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| Exact Mass |
466.24 DPI-201-106
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| CAS # |
97730-95-5
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| 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);
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| SMILES |
N#CC(N1)=CC2=C1C=CC=C2OCC(O)CN3CCN(C(C4=CC=CC=C4)C5=CC=CC=C5)CC3
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| InChi Key |
BYBYHCOEAFHGJL-UHFFFAOYSA-N
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| 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
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| 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
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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 : ~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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