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Chemical Structure| 2086257-77-2 Chemical Structure| 2086257-77-2

Structure of VBIT 4
CAS No.: 2086257-77-2

Chemical Structure| 2086257-77-2

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VBIT-4 is a voltage-dependent anion channel (VDAC) oligomerization inhibitor.

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Product Details of VBIT 4

CAS No. :2086257-77-2
Formula : C21H23ClF3N3O3
M.W : 457.87
SMILES Code : O=C(CC(CO)N1CCN(CC1)C2=CC=C(C=C2)OC(F)(F)F)NC3=CC=C(C=C3)Cl
MDL No. :MFCD32663268
InChI Key :QYSQXVAEFPWMEM-UHFFFAOYSA-N
Pubchem ID :126697666

Safety of VBIT 4

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P313-P337+P313-P362-P403+P233-P405-P501

Related Pathways of VBIT 4

ferroptosis

Isoform Comparison

Biological Activity

Description
VBIT-4 inhibits the oligomerization of voltage-dependent anion channel 1 (VDAC1) with a binding affinity (Kd) of 17 μM. As an inhibitor of apoptosis, it has potential therapeutic applications in conditions associated with apoptosis, including neurodegenerative and cardiovascular diseases [1].

In Vitro:

Cell Line
Concentration Treated Time Description References
HeLa cells 10µM 1 hour VBIT-4 suppressed the release of mtDNA caused by Phb1 knockdown PMC9753472
J774A.1 cells 10µM 1 hour VBIT-4 suppressed the release of mtDNA caused by Phb1 knockdown PMC9753472
NSC-34 cells 15 µM 12 hours VBIT-12 partially prevented the mutant SOD1-induced cell toxicity PMC9456491
mouse lung endothelial cells 5 µM 36 hours VBIT-4 prevented hyperglycemia-induced cell death and mitochondrial dysfunction, inhibiting spontaneous MPT pore opening and ROS generation. PMC10376467
Rat cortical neurons 10 μM 6, 24, 48 hours VBIT-4 prevented Aβ-induced VDAC1 overexpression and apoptotic cell death PMC9795455
Endog−/− MEFs 10 μM VBIT-4 decreased cmtDNA levels and ISG expression PMC8325171
MDA231 10 μM VBIT-4 induces VDAC1 monomerization and promotes PRKN-mediated polyubiquitination PMC10392732
MDA468 10 μM VBIT-4 induces VDAC1 monomerization and promotes PRKN-mediated polyubiquitination PMC10392732

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MpJ- Faslpr lupus-prone mice 10 μM not specified VBIT-4 ameliorated lupus-like symptoms, including the reduction of skin lesions, renal immune complex deposition, proteinuria, anti-dsDNA antibody, antinuclear antibody, IgG, and cell-free mtDNA levels PMC8325171
Mice SOD1G93A mutant mice Intraperitoneal injection 26 mg/kg Every other day for 12 weeks VBIT-12 significantly improved muscle endurance in SOD1G93A mutant mice PMC9456491
C57BL/6 mice DSS-induced colitis model Drinking water 20 mg/kg From day 2 or day 5 until day 14 VBIT-12 significantly alleviated DSS-induced colitis pathology, inhibited inflammatory cell infiltration, apoptosis, mtDNA release, and NLRP3 inflammasome activation, and reduced the inflammatory response PMC8821898
Mice 5 × FAD mouse model Drinking water 20 mg/kg Twice a week for 5 months VBIT-4 prevented cognitive decline, neuronal loss, neuroinflammation, and neuro-metabolic dysfunctions PMC9795455

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.92mL

2.18mL

1.09mL

21.84mL

4.37mL

2.18mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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