| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Vinpocetine (formerly RGH-4405; AY-27,255; AY27,255, RGH4405, TCV-3B, Cavinton, Intelectol; Ethyl apovincaminate) is a synthetic derivative of the vinca alkaloid vincamine which is a natural product extracted from either the seeds of Voacanga africana or the leaves of Vinca minor as well as the lesser periwinkle plant. It is a selective voltage-sensitive sodium channel blocker for the treatment of stroke, vascular dementia and Alzheimer's disease. Vinpocetine has been reported to have a selective and noncompetitive inhibition of Ca2+ PDE and thus regulate cyclic GMP levels in smooth muscle. In addition, vinpocetine has been revealed to inhibit the activities of three resolvable PDE in the cytosol of rat aorta with Ki values of 14±2μM, >1000μM and >1000μM for Ca2+ PDE(+)CaM, cGMP PDE and cAMP PDE, respectively.
| ln Vitro |
Vinpocetine (5-50 μM; 7 hours; VSMC, HUVEC, A549 cells, and RAW264.7 cells) potently suppresses TNF-α-induced NF-κB-dependent transcriptional activity in a dose-dependent manner, with an approximate IC50 value of 25 μM. Vinpocetine has no substantial effect on cell viability [1]. Vinpocetine (50 μM; 7 hours; VSMC, HUVEC, A549 cells, and RAW264.7 cells) substantially suppresses TNF-α-induced TNF-α, IL-1β, IL-8, MCP-1, VCAM- in different cell types 1. Upregulation of ICAM-1 and MIP-2 transcripts [1].
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| ln Vivo |
In mouse models of α- or LPS-induced lung inflammation, vinpocetine (2.5–10 mg/kg; i.p.; C57BL/6 mice) effectively reduces TNF–Interstitial infiltration of polymorphonuclear leukocytes and inhibits the upregulation of pro-inflammatory mediators, such as TNF-α, IL-1β, and MIP-2 [1].
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| Cell Assay |
RT-PCR[1]
Cell Types: VSMCs, HUVECs, A549 cells and RAW264.7 cells Tested Concentrations: 50 μM Incubation Duration: 7 hrs (hours) Experimental Results: 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. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 mice (8 weeks of age)[1]
Doses: 2.5 mg/kg, 5 mg/kg, and 10 mg/kg Route of Administration: intraperitoneal (ip)injection Experimental Results: Inhibited TNF-α- or LPS-induced up- Regulation of proinflammatory mediators, including TNF-α, IL-1β, and MIP-2, and diminished interstitial infiltration of polymorphonuclear leukocytes in a mouse model of TNF-α- or LPS-induced lung inflammation. |
| References |
[1]. Kye-Im Jeon et al. Vinpocetine inhibits NF-κB-dependent inflammation via an IKK-dependent but PDE-independent mechanism PNAS May 25, 2010 vol. 107 no. 21 9795-9800
[2]. Patyar S, et al. Role of vinpocetine in cerebrovascular diseases. Pharmacol Rep. 2011;63(3):618-28. [3]. Alexandre E. Medina Vinpocetine as a potent antiinflammatory agent PNAS June 1, 2010, Vol. 107, No. 22 9921-9922. |
| Molecular Formula |
C22H26N2O2
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| Molecular Weight |
350.45
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| CAS # |
42971-09-5
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| Related CAS # |
Vinpocetine-d5;2734920-39-7
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| SMILES |
O(C([H])([H])C([H])([H])[H])C(C1=C([H])[C@@]2(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])C([H])([H])N3C([H])([H])C([H])([H])C4C5=C([H])C([H])=C([H])C([H])=C5N1C=4[C@]32[H])=O
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| InChi Key |
DDNCQMVWWZOMLN-IRLDBZIGSA-N
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| InChi Code |
InChI=1S/C22H26N2O2/c1-3-22-11-7-12-23-13-10-16-15-8-5-6-9-17(15)24(19(16)20(22)23)18(14-22)21(25)26-4-2/h5-6,8-9,14,20H,3-4,7,10-13H2,1-2H3/t20-,22+/m1/s1
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| Chemical Name |
ethyl (41S,13aS)-13a-ethyl-2,3,41,5,6,13a-hexahydro-1H-indolo[3,2,1-de]pyrido[3,2,1-ij][1,5]naphthyridine-12-carboxylate
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.62 mg/mL (1.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 6.2 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. Solubility in Formulation 2: ≥ 0.62 mg/mL (1.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 6.2 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.62 mg/mL (1.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8535 mL | 14.2674 mL | 28.5347 mL | |
| 5 mM | 0.5707 mL | 2.8535 mL | 5.7069 mL | |
| 10 mM | 0.2853 mL | 1.4267 mL | 2.8535 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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