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| Targets |
Diperdipine targets voltage-dependent calcium channels, blocking calcium influx into vascular smooth muscle and cardiac cells. This leads to vasodilation, reduced systemic vascular resistance, and decreased cardiac workload. The compound has potential for the treatment of angina pectoris and hypertension.
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| ln Vitro |
In vitro, diperdipine functions as a calcium channel antagonist. It blocks voltage-dependent calcium channels, reducing calcium influx. This action is consistent with its in vivo cardiovascular effects. The compound's dihydropyridine structure is characteristic of this class of calcium channel blockers.
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| ln Vivo |
Diperdipine, also known as YS-201, improves left ventricular ejection fraction, stroke index, and systemic vascular resistance. Mean pulmonary artery pressure and wedge pressure did not change considerably, whereas right atrial and left ventricular end-diastolic pressures did slightly rise, probably due to improved venous return. On the other hand, a rise in the left ventricular end-diastolic volume index following dipedipine injection unmistakably points to an increase in preload [1]. Following oral and intravenous dosages, the absolute bioavailability was determined to be 18.7%. The excretion of bile makes up only 0.1% of the entire clearance of dipidipine; it has no effect on the drug's overall removal. Dipedipine's bioavailability rose to 44.3% following intraportal administration, suggesting that the medication is excreted at the prehepatic location [2]. Mice and rats who received a single gavage dosage of dipidipine experienced intolerance reactions, which began at the lowest tested dose levels of 200 mg/kg bwpo for mice and 250 mg/kg bwpo for rats. Toxic effects in rats started at oral dosages of 15 mg/kg body weight/day [3].
In vivo, diperdipine markedly reduces systemic vascular resistance and improves stroke index and left ventricular ejection fraction. Mean pulmonary artery pressure and wedge pressure did not change considerably, whereas right atrial and left ventricular end-diastolic pressures did slightly rise, probably due to improved venous return. It does not affect left ventricular contractility. |
| Enzyme Assay |
In vitro receptor binding assays for diperdipine typically use membrane preparations from cells expressing voltage-dependent calcium channels. Radiolabeled dihydropyridine ligands are displaced by increasing concentrations of the compound to determine binding affinity. Non-specific binding is determined in the presence of excess unlabeled ligand. Functional assays measure the compound's ability to inhibit calcium influx.
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| Cell Assay |
Cell-based functional assays for diperdipine involve measuring calcium influx in cells expressing voltage-dependent calcium channels. Cells are loaded with a calcium-sensitive dye and stimulated with depolarizing agents. The inhibition of calcium influx by the compound is measured. IC50 values are calculated from dose-response curves. The compound's effects on vascular smooth muscle cells can also be assessed.
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| Animal Protocol |
In vivo animal studies for diperdipine typically involve intravenous administration to animal models of hypertension or angina. Hemodynamic parameters such as blood pressure, heart rate, and cardiac output are measured. The compound's ability to reduce systemic vascular resistance and improve cardiac function is assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of diperdipine are characteristic of dihydropyridine calcium channel antagonists. Following intravenous administration, it is rapidly distributed to tissues. Metabolism occurs in the liver. Excretion occurs through renal pathways. The compound has a molecular weight of 457.52.
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| Toxicity/Toxicokinetics |
The toxicological profile of diperdipine is consistent with dihydropyridine calcium channel antagonists. Common side effects include headache, dizziness, and flushing. The compound should be used with caution in patients with heart failure or hypotension. Detailed toxicity data from clinical trials is limited as development was discontinued.
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| References |
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| Additional Infomation |
Diperdipine (YS-201) is a dihydropyridine-type calcium channel antagonist that was previously in clinical trials for the treatment of angina pectoris and hypertension. It is not currently approved for clinical use. The compound is a valuable research tool for studying calcium channel pharmacology and cardiovascular function.
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| Molecular Formula |
C24H31N3O6
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|---|---|
| Molecular Weight |
457.527
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| Exact Mass |
457.221
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| CAS # |
108852-42-2
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| PubChem CID |
130588
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.207g/cm3
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| Boiling Point |
593.9ºC at 760 mmHg
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| Flash Point |
313ºC
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| Vapour Pressure |
4.47E-14mmHg at 25°C
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| Index of Refraction |
1.556
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| LogP |
4.211
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
33
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| Complexity |
810
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LBSRZVRITCRLIU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H31N3O6/c1-4-32-23(28)20-16(2)25-17(3)21(22(20)18-9-8-10-19(15-18)27(30)31)24(29)33-14-13-26-11-6-5-7-12-26/h8-10,15,22,25H,4-7,11-14H2,1-3H3
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| Chemical Name |
3-O-ethyl 5-O-(2-piperidin-1-ylethyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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| Synonyms |
YS201; YS-201; Diperdipine
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.1856 mL | 10.9282 mL | 21.8565 mL | |
| 5 mM | 0.4371 mL | 2.1856 mL | 4.3713 mL | |
| 10 mM | 0.2186 mL | 1.0928 mL | 2.1856 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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