1. Membrane Transporter/Ion Channel
    NF-κB
    Metabolic Enzyme/Protease
  2. Sodium Channel
    IKK
    Phosphodiesterase (PDE)
  3. Vinpocetine

Vinpocetine (Synonyms: Ethyl apovincaminate)

Cat. No.: HY-13295 Purity: 99.77%
Handling Instructions

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.

For research use only. We do not sell to patients.

Vinpocetine Chemical Structure

Vinpocetine Chemical Structure

CAS No. : 42971-09-5

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Description

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[1][2][3].

IC50 & Target

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].
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].

RT-PCR[1]

Cell Line: VSMCs, HUVECs, A549 cells and RAW264.7 cells
Concentration: 50 μM
Incubation Time: 7 hours
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

Vinpocetine (2.5-10 mg/kg; intraperitoneal injection; C57BL/6 mice) potently inhibits TNF-α- or LPS-induced up-regulation of proinflammatory mediators, including TNF-α, IL-1β, and MIP-2, and decreases interstitial infiltration of polymorphonuclear leukocytes in a mouse model of TNF-α- or LPS-induced lung inflammation[1].

Animal Model: C57BL/6 mice (8 weeks of age)[1]
Dosage: 2.5 mg/kg, 5 mg/kg, and 10 mg/kg
Administration: Intraperitoneal injection
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.
Clinical Trial
Molecular Weight

350.45

Formula

C₂₂H₂₆N₂O₂

CAS No.

42971-09-5

SMILES

CCOC(C1=C[[email protected]]2(CC)CCCN3CCC(C4=C(C=CC=C4)N51)=C5[[email protected]]23[H])=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.25 mg/mL (17.83 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.62 mg/mL (1.77 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.77%

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Keywords:

VinpocetineEthyl apovincaminateSodium ChannelIKKPhosphodiesterase (PDE)Na channelsNa+ channelsIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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