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VBIT-4

SKU: orb1708263

Description

VBIT-4 is a small molecule inhibitor of VDAC1 oligomerization with a Kd of 17 µM. It is a research tool for studying apoptosis in models of neurodegenerative and cardiovascular diseases, showing therapeutic potential in both in vitro and in vivo experimental systems.

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number2086257-77-2
MW457.87
Purity99.93% (May vary between batches)
FormulaC21H23ClF3N3O3
SMILESC(CC(NC1=CC=C(Cl)C=C1)=O)(CO)N2CCN(CC2)C3=CC=C(OC(F)(F)F)C=C3
TargetVDAC
SolubilityDMSO:245 mg/mL (535.09 mM);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)

Bioactivity

Target IC50
HEK293 cells:2.9 µM|VDAC1:17 Μm (kd)|VDAC1:1.9 ± 0.08 μM|Cytochrome c:1.8 ± 0.24 μM
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.
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

VBIT 4, VBIT4, VBIT-4, VDAC1
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Key Properties

No computed properties available.

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Protocol Information

VBIT-4 (orb1708263)

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% DMSO +
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% Tween 80 +
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Available Sizes

Select a size below

1 mg
¥ 1,430.00
5 mg
¥ 2,730.00
1 ml x 10 mM (in DMSO)
¥ 2,860.00
10 mg
¥ 4,290.00
25 mg
¥ 7,020.00
50 mg
¥ 11,310.00
100 mg
¥ 14,690.00
200 mg
¥ 19,760.00
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