| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The primary targets of Prodipine hydrochloride are L-type calcium channels and dipeptidyl peptidase IV (DPP IV). As a calcium channel blocker, it inhibits calcium influx into vascular smooth muscle cells, reducing contraction and leading to vasodilation. As a DPP IV inhibitor, it is a slow-binding irreversible inhibitor of this enzyme. Its IC50 values are 4.5 uM for purified rabbit DPP IV and 30 uM for plasma DPP IV. This dual mechanism makes it a unique compound for studying both cardiovascular and metabolic pathways.
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| ln Vitro |
Prodipine, a diphenylphosphonate derivative, was chosen from the list of slow-binding irreversible inhibitors of this enzyme. Prodipine's IC50 values for rabbit pure DPP IV and plasma DPP IV are 4.5 and 30 μM, respectively [1].
In vitro, Prodipine is a diphenyl-phosphonate derivative selected from a group of slow-binding irreversible inhibitors of DPP IV. Its IC50 values are 4.5 uM for purified rabbit DPP IV and 30 uM for plasma DPP IV. As a calcium channel blocker, it inhibits calcium influx into vascular smooth muscle cells. These activities make it a valuable tool for studying both calcium channel function and DPP IV inhibition in cell-based assays. Its effects on these two distinct targets are concentration-dependent. |
| ln Vivo |
A single intravenous injection of 10 mg prodipine or normal saline was given to male rabbits weighing 3–4 kg. The plasma DPP IV activity was less than 20% of the pre-injection value after an hour, and it stayed that way for the duration of the 24-hour observation period. In treated animals, there was a significant and prolonged suppression of plasma DPP IV activity (1, 5 or 10 mg). Half of the pre-treatment DPP IV activity is reached in 5 to 8 days, and recovery takes more than 20 days on average [1].
In vivo, Prodipine hydrochloride is used to treat hypertension and angina by acting as a calcium channel blocker. Systemic treatment with Prodipine leads to inhibition of plasma DPP IV activity and also decreases tissue DPP IV activity in circulating mononuclear cells, kidney cortex, thymus, spleen, lung, and liver. This demonstrates its bioavailability and ability to inhibit DPP IV in various tissues. It lowers blood pressure by inducing vasodilation. |
| Enzyme Assay |
Cell-free enzyme assays for Prodipine hydrochloride typically assess its inhibition of DPP IV. A standard protocol involves incubating the enzyme (purified rabbit DPP IV or plasma) with a fluorogenic substrate (e.g., Gly-Pro-AMC) and varying concentrations of Prodipine in a reaction buffer. The reaction is carried out at 37degC, and the release of the fluorescent AMC is measured over time. The IC50 is determined from the dose-response curve. This assay characterizes its potency as a DPP IV inhibitor.
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| Cell Assay |
For in vitro cellular experiments, cells such as vascular smooth muscle cells are cultured in appropriate media. Cells are treated with Prodipine hydrochloride at various concentrations (typically 0.1-100 uM). Intracellular calcium levels are measured using fluorescent calcium indicators (e.g., Fluo-4) to assess its calcium channel blocking activity. For DPP IV studies, cells expressing DPP IV are treated with the compound, and enzyme activity is measured using a fluorogenic substrate. These experiments define its dual activity in a cellular context.
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| Animal Protocol |
In vivo animal experiments with Prodipine hydrochloride are conducted in rodent models of hypertension. A common protocol involves administering the compound orally or intraperitoneally at various doses (e.g., 1-50 mg/kg) to spontaneously hypertensive rats. Blood pressure is measured using a tail-cuff or telemetry system. The compound's antihypertensive effect is assessed by the reduction in blood pressure over time. For DPP IV studies, plasma and tissue samples are collected, and DPP IV activity is measured.
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| ADME/Pharmacokinetics |
Prodipine hydrochloride has a molecular weight of 315.9 g/mol. It is a small molecule that is likely to have good oral bioavailability. It is soluble in DMSO and should be stored as a powder at -20degC. Its pharmacokinetic properties, including half-life and tissue distribution, would need to be characterized for therapeutic development. It is for research use only and not for human therapeutic use.
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| Toxicity/Toxicokinetics |
The toxicity profile of Prodipine hydrochloride has not been extensively characterized. As a calcium channel blocker, it can cause hypotension, bradycardia, and other cardiovascular effects at high doses. As a DPP IV inhibitor, it may have effects on glucose metabolism and immune function. However, it is generally well-tolerated at therapeutic doses. It is for research use only and not for human therapeutic use. It should be handled with standard laboratory precautions.
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| References | |
| Additional Infomation |
Prodipine hydrochloride is a diphenyl-phosphonate derivative that acts as both a calcium channel blocker and an inhibitor of dipeptidyl peptidase IV (DPP IV). As a calcium channel blocker, it is used to treat hypertension and angina. As a DPP IV inhibitor, it has IC50 values of 4.5 uM and 30 uM for purified and plasma DPP IV, respectively. It is a valuable research tool for studying cardiovascular and metabolic pathways.
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| Molecular Formula |
C20H25N.HCL
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|---|---|
| Molecular Weight |
315.88014
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| Exact Mass |
315.175
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| CAS # |
31314-39-3
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| Related CAS # |
31314-38-2;31314-39-3 (HCl);
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| PubChem CID |
3030531
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| Appearance |
Off-white to yellow solid powder
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| LogP |
5.216
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
282
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZFCBOUXJVGNRIF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H25N.ClH/c1-17(2)21-15-13-20(14-16-21,18-9-5-3-6-10-18)19-11-7-4-8-12-19;/h3-12,17H,13-16H2,1-2H3;1H
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| Chemical Name |
4,4-diphenyl-1-propan-2-ylpiperidine;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 | 3.1658 mL | 15.8288 mL | 31.6576 mL | |
| 5 mM | 0.6332 mL | 3.1658 mL | 6.3315 mL | |
| 10 mM | 0.3166 mL | 1.5829 mL | 3.1658 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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