Conditionnement : 1mLx10mM(inDMSO)
Synonyms:
| 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, VDAC1:17 Μm (kd), Cytochrome c:1.8 ± 0.24 μM, 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] |
| Molecular Weight | 457.87 |
| Formula | C21H23ClF3N3O3 |
| Cas No. | 2086257-77-2 |
| Smiles | C(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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 245 mg/mL (535.09 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 5% DMSO+40% PEG300+5% Tween 80+50% Saline: 2 mg/mL (4.37 mM) 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
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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