Papaveroline
Based on 1 Customer Validation
Papaveroline is a Fyn tyrosine kinase inhibitor, Na+,K+-ATPase inhibitor with an IC50 of 0.20 mM, Mg2+-ATPase inhibitor, K+-activated pNPPase inhibitor with an IC50 of 1.51 mM, and apoptosis inducer. Papaveroline binds to the active site of Fyn tyrosine kinase and forms stable interactions with pocket amino acid residues. Papaveroline induces cell apoptosis, produces pycnotic and fragmented cell nuclei, and does not reduce intracellular ATP levels. Papaveroline is a dopamine-derived neurotoxin candidate associated with the pathogenesis of Parkinson's disease. Papaveroline can be used in the research of Alzheimer's disease and Parkinson's disease.
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- CAS No.: 574-77-6
- Formule: C16H13NO4
- Masse moléculaire:283.28
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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Na+,K+-ATPase 0.2 mM (IC50, rat brain microsomal) |
K+-activated pNPPase 1.51 mM (IC50, rat brain microsomal) |
In Vitro
Papaveroline inhibits rat brain microsomal K+-activated pNPPase with an IC50 of 1.51 mM, which is less potent than its inhibition of rat brain microsomal Na+,K+-ATPase[2].
Papaveroline (75-100% inhibition; 10 min)-mediated inhibition of rat brain microsomal Na+,K+-ATPase is freely reversible, as enzyme activity returns to control levels following washing and resuspension of the enzyme[2].
Papaveroline (200-400 μM) acts as a simple linear noncompetitive inhibitor of rat brain microsomal Na+,K+-ATPase with respect to ATP, exhibiting an apparent Ki of 380.00 μM[2].
Papaveroline (300 μM) decreases the apparent affinity of rat brain microsomal Na+,K+-ATPase for Na+ by increasing the K0.5 by 65% without altering cooperative binding at the Na+ site or the enzyme's Vmax[2].
Papaveroline inhibits beef cardiac Na+,K+-ATPase with an IC50 of 0.76 mM, which is less potent than its inhibition of rat brain microsomal Na+,K+-ATPase[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human dopaminergic neuroblastoma SH-SY5Y cells
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Concentration:100 μM; 250 μM; 500 μM
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Incubation Time:18 h
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Result:Induced apoptosis in 69.19% of cells, with necrosis in 6.99% of cells at 100 μM.
Induced apoptosis in 83.07% of cells, with necrosis in 6.47% of cells at 250 μM.
Induced apoptosis in 32.3% of cells, with necrosis in 67.88% of cells at 500 μM.
Caused condensed cell bodies with retarded neurites, and condensed/fragmented nuclei typical of apoptosis after Hoechst 33342 staining.
Chemical Information
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CAS No. 574-77-6
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Appearance Solid
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Masse moléculaire 283.28
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Formule C16H13NO4
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SMILES
OC1=CC=C(CC2=NC=CC3=C2C=C(O)C(O)=C3)C=C1O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (353.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (8.83 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
Références
[1]. Bhat SS, et al. Computational Insights into Papaveroline as an In Silico Drug Candidate for Alzheimer's Disease via Fyn Tyrosine Kinase Inhibition. Molecular biotechnology. 2025 Jul;67(7):2743-2757. [Content Brief]
[2]. Meyerson LR, et al. Isoquinoline alkaloids. Inhibitory actions on cation-dependent ATP-phosphohydrolases. Neurochemical research. 1978 Apr;3(2):239-57. [Content Brief]
[3]. Maruyama W, et al. Dopaminergic neurotoxins, 6,7-dihydroxy-1-(3', 4'-dihydroxybenzyl)-isoquinolines, cause different types of cell death in SH-SY5Y cells: apoptosis was induced by oxidized papaverolines and necrosis by reduced tetrahydropapaverolines. Neuroscience letters. 2000 Sep 15;291(2):89-92. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.5301 mL | 17.6504 mL | 35.3008 mL | 88.2519 mL |
| 5 mM | 0.7060 mL | 3.5301 mL | 7.0602 mL | 17.6504 mL | |
| 10 mM | 0.3530 mL | 1.7650 mL | 3.5301 mL | 8.8252 mL | |
| 15 mM | 0.2353 mL | 1.1767 mL | 2.3534 mL | 5.8835 mL | |
| 20 mM | 0.1765 mL | 0.8825 mL | 1.7650 mL | 4.4126 mL | |
| 25 mM | 0.1412 mL | 0.7060 mL | 1.4120 mL | 3.5301 mL | |
| 30 mM | 0.1177 mL | 0.5883 mL | 1.1767 mL | 2.9417 mL | |
| 40 mM | 0.0883 mL | 0.4413 mL | 0.8825 mL | 2.2063 mL | |
| 50 mM | 0.0706 mL | 0.3530 mL | 0.7060 mL | 1.7650 mL | |
| 60 mM | 0.0588 mL | 0.2942 mL | 0.5883 mL | 1.4709 mL | |
| 80 mM | 0.0441 mL | 0.2206 mL | 0.4413 mL | 1.1031 mL | |
| 100 mM | 0.0353 mL | 0.1765 mL | 0.3530 mL | 0.8825 mL |
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