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Chemical Structure| 6501-72-0 Chemical Structure| 6501-72-0

Structure of VGX-1027
CAS No.: 6501-72-0

Chemical Structure| 6501-72-0

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VGX-1027 is an orally active immunomodulatory agent that primarily targets macrophages, it can inhibit TNF-α secretion via interference of macrophage toll-like receptor (TLR) 4 and TLR 2/6 signaling pathway. VGX-1027 also reduces the secretion of pro-inflammatory cytokines IL1-β, IL-10 and IFN-γ.

Synonyms: GIT 27

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Product Details of VGX-1027

CAS No. :6501-72-0
Formula : C11H11NO3
M.W : 205.21
SMILES Code : O=C(O)CC1CC(C2=CC=CC=C2)=NO1
Synonyms :
GIT 27
MDL No. :MFCD08696167
InChI Key :MUFJHYRCIHHATF-UHFFFAOYSA-N
Pubchem ID :10798271

Safety of VGX-1027

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Peripheral blood mononuclear cells 10 µM 48 hours To study the immunomodulatory effects of VGX-1027 on LPS-induced Toll-like receptor 4 activation, results showed that VGX-1027 significantly altered the gene expression profile, particularly downregulating genes involved in antigen processing and presentation. Immunology. 2014 Aug;142(4):594-602
HepG2 cells 1000, 500, 250 nM 5 hours To evaluate the protective effects of GIT-27NO and VGX-1027 against H2O2-induced oxidative stress. GIT-27NO significantly counteracted the toxic effects of H2O2, while VGX-1027 showed only mild protection at the highest concentration. Int J Immunopathol Pharmacol. 2019 Jan-Dec;33:2058738419862736
Human podocytes 10 μg/ml 72 hours To investigate the effect of GIT27 on podocyte apoptosis induced by sera with high LPS activity, results showed that GIT27 pretreatment prevented downregulation of PDK1 expression and reduced apoptosis. Cell Death Dis. 2015 May 7;6(5):e1752

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB-C mice LPS-induced podocyte injury and proteinuria model Intraperitoneal injection 20 mg/kg 24 hours before and 2 hours after LPS challenge To evaluate the protective effect of GIT27 on LPS-induced podocyte injury, results showed that GIT27 treatment prevented the decrease in PDK1 expression and podocyte apoptosis. Cell Death Dis. 2015 May 7;6(5):e1752
NZB/NZW F1 mice Systemic lupus erythematosus model Intraperitoneal injection 20 mg/kg Daily for 20 weeks To evaluate the effects of VGX-1027 on the systemic lupus erythematosus model, results showed that VGX-1027 significantly improved survival, reduced proteinuria and kidney pathology, and decreased anti-dsDNA antibody and cytokine production. Immunology. 2014 Aug;142(4):594-602
Lewis rats Endotoxin-induced uveitis (EIU) model Intraperitoneal injection 25 mg/kg Single dose, at 30 min, 6 h or 12 h after LPS injection VGX-1027 significantly alleviated clinical, histological and laboratory signs of EIU when administered within 6 h after LPS challenge Br J Pharmacol. 2008 Nov;155(5):722-30
Mice Controlled cortical impact (TBI) model Tail vein injection 50 mg/kg Single dose, 4 hours post-injury To evaluate the effect of VGX-1027 on cerebral edema after TBI. A 4h post-treatment significantly attenuated edema, while pre-treatment or 1h post-treatment was ineffective. Glia. 2014 Jan;62(1):26-38

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00627120 Healthy PHASE1 COMPLETED - SNBL Clinical Pharmacology Cen... More >>ter, Baltimore, Maryland, 21201, United States Less <<
NCT00760396 Healthy PHASE1 COMPLETED 2025-04-09 SNBL Clinical Pharmacology Cen... More >>ter, Inc., Baltimore, Maryland, 21201, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.87mL

0.97mL

0.49mL

24.37mL

4.87mL

2.44mL

48.73mL

9.75mL

4.87mL

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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