Vinpocetine
Based on 8 publication(s) in Google Scholar
Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+ channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.
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- Pureza : 99.57%
- No. CAS: 42971-09-5
- Fòrmula: C22H26N2O2
- Peso molecular:350.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Vinpocetine
More- Nat Commun. 2023 Jun 3;14(1):3224. [Abstract]
- PLoS Biol. 2024 Mar 25;22(3):e3002565. [Abstract]
- Front Cell Dev Biol. 2021 Feb 4:8:616590. [Abstract]
- Neuroscience. 2023 Aug 21:526:74-84. [Abstract]
- J Cancer Res Clin Oncol. 2023 Aug;149(10):7703-7716. [Abstract]
- J Taibah Univ Med Sci. 2023 Sep 20;19(1):35-53. [Abstract]
- J Investig Med. 2022 Aug;70(6):1358-1364. [Abstract]
- The Hong Kong Polytechnic University. 2023 Aug.
Actividad biológica
Descripciòn
IC50 & Target
[1]|
IKK 17.17 μM (IC50) |
In Vitro
Vinpocetine (5-50 μM; 7 hours; VSMCs, HUVECs, A549 cells and RAW264.7 cells) potently inhibits TNF-α-induced NF-κB-dependent transcriptional activity in a dose-dependent manner with an approximate IC50 value of 25 μM. Vinpocetine do not have a significant effect on cell viability[1].
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Vinpocetine (50 μM; 7 hours; VSMCs, HUVECs, A549 cells and RAW264.7 cells) potently inhibits TNF-α-induced up-regulation of TNF-α, IL-1β, IL-8, MCP-1, VCAM-1, ICAM-1and MIP-2 transcripts in several cell types[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:VSMCs, HUVECs, A549 cells and RAW264.7 cells
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Concentration:50 μM
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Incubation Time:7 hours
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Result:Inhibited TNF-α-induced up-regulation of TNF-α, IL-1β, IL-8, MCP-1, VCAM-1, ICAM-1and MIP-2 transcripts in several cell types.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (8 weeks of age)[1]
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Dosage:2.5 mg/kg, 5 mg/kg, and 10 mg/kg
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Administration:Intraperitoneal injection
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Result:Inhibited TNF-α- or LPS-induced up-regulation of proinflammatory mediators, including TNF-α, IL-1β, and MIP-2, and decreased interstitial infiltration of polymorphonuclear leukocytes in a mouse model of TNF-α- or LPS-induced lung inflammation.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 42971-09-5
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Appearance Solid
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Peso molecular 350.45
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Fòrmula C22H26N2O2
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Color White to off-white
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SMILES
CCOC(C1=C[C@]2(CC)CCCN3CCC(C4=C(C=CC=C4)N51)=C5[C@]23[H])=O
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Synonyms
Ethyl apovincaminate
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Nat Commun
2023 Jun 3;14(1):3224. PMID: 37270609 -
PLoS Biol
The scale of zebrafish pectoral fin buds is determined by intercellular K+ levels and consequent Ca2+-mediated signaling via retinoic acid regulation of Rcan2 and Kcnk5b. [Abstract]2024 Mar 25;22(3):e3002565. PMID: 38527087 -
Front Cell Dev Biol
Inhibition of PDE1-B by Vinpocetine Regulates Microglial Exosomes and Polarization Through Enhancing Autophagic Flux for Neuroprotection Against Ischemic Stroke. [Abstract]2021 Feb 4:8:616590. PMID: 33614626 -
Neuroscience
Neuroprotective Effects of Vinpocetine against Ischemia-Reperfusion Injury via Inhibiting NLRP3 Inflammasome Signaling Pathway. [Abstract]2023 Aug 21:526:74-84. PMID: 37290685 -
J Cancer Res Clin Oncol
YAP inhibitor verteporfin suppresses tumor angiogenesis and overcomes chemoresistance in esophageal squamous cell carcinoma. [Abstract]2023 Aug;149(10):7703-7716. PMID: 37000262 -
J Taibah Univ Med Sci
Attenuated effects of topical vinpocetine in an imiquimod-induced mouse model of psoriasis. [Abstract]2023 Sep 20;19(1):35-53. PMID: 37868105 -
J Investig Med
Vinpocetine enhances cisplatin sensitivity of non-small cell lung cancer cells by reducing the nuclear factor erythroid 2-related factor 2 signaling. [Abstract]2022 Aug;70(6):1358-1364. PMID: 35580917 -
Solvente y solubilidad
In Vitro:
Ethanol : 14.29 mg/mL (40.78 mM; Need ultrasonic)
DMSO : 6.25 mg/mL (17.83 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 0.62 mg/mL (1.77 mM); Clear solution
This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 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: ≥ 0.62 mg/mL (1.77 mM); Clear solution
This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 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.
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureza y Documentación
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Ficha de datos (288 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 2.8535 mL | 14.2674 mL | 28.5347 mL | 71.3369 mL |
| 5 mM | 0.5707 mL | 2.8535 mL | 5.7069 mL | 14.2674 mL | |
| 10 mM | 0.2853 mL | 1.4267 mL | 2.8535 mL | 7.1337 mL | |
| 15 mM | 0.1902 mL | 0.9512 mL | 1.9023 mL | 4.7558 mL | |
| Ethanol | 20 mM | 0.1427 mL | 0.7134 mL | 1.4267 mL | 3.5668 mL |
| 25 mM | 0.1141 mL | 0.5707 mL | 1.1414 mL | 2.8535 mL | |
| 30 mM | 0.0951 mL | 0.4756 mL | 0.9512 mL | 2.3779 mL | |
| 40 mM | 0.0713 mL | 0.3567 mL | 0.7134 mL | 1.7834 mL |
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