VBIT-4 [2086257-77-2]

Cat# NB-64-04846-10mg

Size : 10mg

Brand : Neo Biotech

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VBIT-4

VBIT-4 is a voltage-dependent anion channel 1 (VDAC1) oligomerization inhibitor (Kd: 17 μM). VBIT-4 can be used for therapeutic purposes in apoptosis-associated disorders (such as neurodegenerative and cardiovascular diseases).

VBIT-4

Product Introduction

Bioactivity
Description
VBIT-4 is a voltage-dependent anion channel 1 (VDAC1) oligomerization inhibitor (Kd: 17 μM). VBIT-4 can be used for therapeutic purposes in apoptosis-associated disorders (such as neurodegenerative and cardiovascular diseases).
Targets&IC50
HEK293 cells:2.9 µM, Cytochrome c:1.8 ± 0.24 μM, VDAC1:17 Μm (kd), VDAC1:1.9 ± 0.08 μM
In vitro
VBIT-4 targets the mitochondrial protein VDAC1, inhibits apoptosis and defends against mitochondrial dysfunction. VBIT-4 (0.1-10 μM) inhibits VDAC1 oligomerization, Cyto c release from mitochondria and apoptosis (in HEK-293 cells , IC50s of 1.9±0.08 μM, 1.8±0.24 μM, and 2.9±0.12 μM, respectively).VBIT-4 offer a therapeutic strategy for treating different diseases associated with enhanced apoptosis and point to VDAC1 as a promising target for therapeutic intervention.
In vivo
METHODS: To test the effect on Alzheimer's disease, VBIT-4 (25 mg/kg) was injected intraperitoneally into APP/PS1 mice once daily for four weeks.
RESULTS: VDAC1 was significantly up-regulated in APP/PS1 mice and decreased after VBIT-4 treatment; GPX4 expression was decreased in APP/PS1 mice and restored by VBIT-4 treatment; MWM test showed that APP/PS1 mice had a longer latency to find the plateau; VBIT-4 treatment significantly decreased the latency to find the plateau in APP/PS1 mice. VBIT-4 treatment significantly reduced the latency of platform finding in APP/PS1 mice. [3]
Chemical Properties
Molecular Weight457.87
FormulaC21H23ClF3N3O3
Cas No.2086257-77-2
SmilesC(CC(NC1=CC=C(Cl)C=C1)=O)(CO)N2CCN(CC2)C3=CC=C(OC(F)(F)F)C=C3
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 45 mg/mL (98.28 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4.5 mg/mL (9.83 mM), Solution.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1840 mL10.9201 mL21.8403 mL109.2013 mL
5 mM0.4368 mL2.1840 mL4.3681 mL21.8403 mL
10 mM0.2184 mL1.0920 mL2.1840 mL10.9201 mL
20 mM0.1092 mL0.5460 mL1.0920 mL5.4601 mL
50 mM0.0437 mL0.2184 mL0.4368 mL2.1840 mL

Sci Citations

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