| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Pranidipine targets voltage-dependent L-type calcium channels, which are present in vascular smooth muscle and cardiac muscle. It has a high affinity for Ca channels or T-tubule membranes. By blocking these channels, it inhibits calcium influx, leading to vasodilation and reduced peripheral vascular resistance. It also enhances nitric oxide-induced relaxation of the rat aorta through a cyclic GMP-independent mechanism.
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| ln Vitro |
In vitro, pranidipine acts as a long-acting calcium channel antagonist. It has a high affinity for Ca channels or T-tubule membranes. It enhances cyclic GMP-independent nitric oxide-induced relaxation of the rat aorta. These activities have been demonstrated in isolated tissue preparations and cell-based assays, confirming its vasodilatory and antihypertensive effects.
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| ln Vivo |
In vivo, pranidipine is used as an antihypertensive agent for the treatment of hypertension. Its long-lasting effects make it suitable for once-daily dosing. Its ability to enhance nitric oxide-induced relaxation contributes to its vasodilatory effects. It is approved for use in several countries.
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| Enzyme Assay |
The in vitro receptor binding/functional assay for pranidipine typically involves measuring its ability to inhibit calcium influx through L-type calcium channels. These assays can be performed using radioligand binding studies with membrane preparations or using patch-clamp techniques on cells expressing the channels. Its affinity for Ca channels is determined from displacement studies. Its effects on nitric oxide-induced relaxation are assessed in isolated tissue preparations.
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| Cell Assay |
In vitro cellular assays for pranidipine assess its effects on calcium signaling and vascular smooth muscle function. Vascular smooth muscle cells are treated with pranidipine, and intracellular calcium levels are measured. Its effects on cell contraction and relaxation are assessed in isolated aortic rings. These assays demonstrate the compound's functional activity as a calcium channel blocker and vasodilator.
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| Animal Protocol |
In vivo animal studies for pranidipine have been conducted in animal models of hypertension to evaluate its antihypertensive efficacy. Its effects on blood pressure, heart rate, and vascular function have been assessed. These studies have demonstrated its long-lasting antihypertensive effects and its ability to enhance nitric oxide-induced relaxation.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Known metabolites of praldiprine include dehydropraldiprine, 5-methoxycarbonyl-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid, and β-methylstyrene. Specific pharmacokinetic data for pranidipine are not extensively detailed in the available literature. As a long-acting calcium channel blocker, it is expected to have a prolonged duration of action. It has a logP of 4.2592 and is poorly soluble in water (2.5E-4 g/L at 25 °C). Its pharmacokinetic properties support once-daily dosing for the treatment of hypertension. |
| Toxicity/Toxicokinetics |
Specific toxicity data for pranidipine are not extensively detailed in the available literature. As a dihydropyridine calcium channel blocker, its toxicity profile is likely similar to other drugs in this class, including peripheral edema, headache, dizziness, and flushing. It is intended for research purposes only and is not for human use.
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| References | |
| Additional Infomation |
Pranidipine (CAS 99522-79-9) is a long-acting dihydropyridine calcium channel blocker used as an antihypertensive agent. It has a high affinity for Ca channels and enhances cyclic GMP-independent nitric oxide-induced relaxation of the rat aorta. It was developed in Japan in the 1990s and has been approved for use in several countries. It is a research compound and is not approved for clinical use in all regions.
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| Molecular Formula |
C25H24N2O6
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|---|---|
| Molecular Weight |
448.46800
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| Exact Mass |
448.163
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| CAS # |
99522-79-9
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| PubChem CID |
6436048
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
618.9±55.0 °C at 760 mmHg
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| Melting Point |
140-142ºC
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| Flash Point |
328.1±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.606
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| LogP |
5.35
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
33
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| Complexity |
847
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(C(=C(N1)C)C(=O)OC/C=C/C2=CC=CC=C2)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OC
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| InChi Key |
XTFPDGZNWTZCMF-DHZHZOJOSA-N
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| InChi Code |
InChI=1S/C25H24N2O6/c1-16-21(24(28)32-3)23(19-12-7-13-20(15-19)27(30)31)22(17(2)26-16)25(29)33-14-8-11-18-9-5-4-6-10-18/h4-13,15,23,26H,14H2,1-3H3/b11-8+
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| Chemical Name |
3-O-methyl 5-O-[(E)-3-phenylprop-2-enyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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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 : ~270 mg/mL (~602.05 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (5.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 22.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2298 mL | 11.1490 mL | 22.2980 mL | |
| 5 mM | 0.4460 mL | 2.2298 mL | 4.4596 mL | |
| 10 mM | 0.2230 mL | 1.1149 mL | 2.2298 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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