2. Immunology/Inflammation Cytoskeleton NF-κB Anti-infection
  3. STING Integrin NF-κB SARS-CoV
  4. diABZI-4

diABZI-4 is a STING activator and broad-spectrum antiviral agent with immunostimulatory activity. diABZI-4 triggers the TBK1-IRF3 and NF-κB signaling cascades by inducing STING oligomerization, thereby promoting the production of type I/III interferons and various proinflammatory cytokines. diABZI-4 exhibits broad-spectrum antiviral activity and effectively inhibits the replication of influenza A virus, SARS-CoV-2, herpes simplex virus, and other viruses. diABZI-4 also activates lymphocytes and macrophages to provide significant pre- and post-exposure protection in viral disease models. diABZI-4 can be used to study COVID-19, respiratory viral infections, and related immunopathological mechanisms.

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diABZI-4

diABZI-4 Chemical Structure

CAS No. : 2138299-65-5

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Based on 1 publication(s) in Google Scholar

diABZI-4 Related Antibodies

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  • Biological Activity

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Description

diABZI-4 is a STING activator and broad-spectrum antiviral agent with immunostimulatory activity. diABZI-4 triggers the TBK1-IRF3 and NF-κB signaling cascades by inducing STING oligomerization, thereby promoting the production of type I/III interferons and various proinflammatory cytokines. diABZI-4 exhibits broad-spectrum antiviral activity and effectively inhibits the replication of influenza A virus, SARS-CoV-2, herpes simplex virus, and other viruses. diABZI-4 also activates lymphocytes and macrophages to provide significant pre- and post-exposure protection in viral disease models. diABZI-4 can be used to study COVID-19, respiratory viral infections, and related immunopathological mechanisms[1][2][3][4].

In Vitro

diABZI-4 (50-500 nM; 5-24 h) induces robust expression of innate immune genes, including IFNβ, RSAD2, TNF, IL-6, and TRIM22, in MRC-5 human lung fibroblasts[2].
diABZI-4 (0.007-5 μM; 0.5-3 h) activates STING and stimulates secretion of innate immune cytokines, including IFNβ, IP-10, and IL-6, in primary human nasal epithelial ALI tissues, with short exposures (0.5-1 h) via either apical or basal surfaces sufficient for activation[2].
diABZI-4 (50 nM; 24 h) activates iMacs, as measured by increased CD80 and CD86 expression and pro-inflammatory cytokine secretion, and protects iMacs against IAV infection at 24 h post-infection[2].
diABZI-4 (500 nM; 24 h) induces robust IFNβ secretion in murine bone marrow-derived macrophages following 24 h of treatment[3].
diABZI-4 (500 nM; 15-60 min) induces comparable levels of STING oligomerization in wild-type and Padi4-deficient murine bone marrow-derived macrophages following 15, 30, and 60 min of treatment[3].
diABZI-4 exhibits broad-spectrum in vitro prophylactic antiviral activity against cell line infections with chikungunya virus, influenza A virus (H1N1), and SARS-CoV-2 (Omicron) with EC50 of 10.06 nM, 14.7 nM, and 199 nM, respectively[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

diABZI-4 Related Antibodies

Real Time qPCR[2]

Cell Line: MRC-5 human lung fibroblasts
Concentration: 50 nM, 500 nM
Incubation Time: 5 h, 24 h
Result: Induced significant upregulation of IFNβ, RSAD2, TNF, IL-6, and TRIM22 transcript levels (expressed as fold-change relative to DMSO control) at both 5 and 24 h, with RSAD2 showing the highest fold induction.
In Vivo

diABZI-4 (1 mg/kg; i.p.; single dose) induces robust serum IFN-β production in wild-type mice[1].
diABZI-4 (0.5 mg/kg; retro-orbital; single dose; 1 hour pre-infection) confers 100% survival and eliminates HSV-1-induced disease and viral titers in cGAS-/- mice[1].
diABZI-4 (0.25-0.5 mg/kg; i.n.; single dose; 3 hours pre-infection or 12 hours post-infection) confers 100% survival and eliminates SARS-CoV-2-induced disease, viral replication, and lung pathology in K18-ACE2 mice[1].
diABZI-4 (0.5 mg/kg; i.n.; single dose; 3 hours pre-infection, co-administered with anti-IFNAR antibody) confers protection against SARS-CoV-2 in K18-ACE2 mice through both IFN-dependent and IFN-independent mechanisms[1].
diABZI-4 (0.1 mg/kg; intranasal (i.n.); single administration) provides significant but transient inhibition of IAV replication in the lungs of C57BL/6J mice, with antiviral activity limited to day 1 post infection[2].
diABZI-4 (0.1 mg/kg; intranasal (i.n.); single administration) induces a rapid, transient peak of lung innate immune transcripts and cytokines in C57BL/6J mice, with sustained but declining compound levels in the lungs over 8 days and limited systemic activity[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: K18-ACE2 transgenic mice with COVID-19 infecition model (2B6.Cg-Tg(K18-ACE2)2Prlmn/J) mice (8-12-week-old, male and female)[1]
Dosage: 0.25-0.5 mg/kg
Administration: i.n.; single dose; 3 hours pre-infection or 12 hours post-infection
Result: Provided 100% survival, prevented SARS-CoV-2-induced weight loss, reduced lung expression of SARS-CoV-2 N protein, Nsp14, and ORF1 genes, decreased viral genome copy numbers, and protected against severe lung inflammation and alveolar wall thickening (0.5 mg/kg, 3 hours pre-infection).
Provided 100% survival and prevented SARS-CoV-2-induced weight loss (0.5 mg/kg, 12 hours post-infection).
Provided complete protection from SARS-CoV-2-induced weight loss and lethality (0.25 mg/kg).
Animal Model: C57BL/6J mice (9−10 weeks old, female)[2]
Dosage: 0.1 mg/kg
Administration: intranasal (i.n.); single administration
Result: Peaked induction of host ISG and cytokine transcripts (including IFIT1, MX1, IL-6, CXCL10, ISG15, IFNL, IFNβ, STAT1, TNFα) at 3 hours (0.125 days) post treatment, with selected transcripts remaining elevated but declining over the 8-day study.
Peaked lung cytokine levels (including IFNα, IFNγ, IL-1β, IL-6, IP-10, MCP-1, TNFα) at day 1, remained elevated through day 4, and dropped to near-baseline by day 8.
Detected diABZI-4 in lung homogenates at 3 hours post treatment, with levels declining after 2 days but still measurable at 8 days post treatment.
Detected minimal compound levels and cytokine activation in serum.
Molecular Weight

844.36

Formula

C40H50ClN13O6
CAS No.
Appearance

Solid

Color

Light yellow to light brown

SMILES

O=C(C1=CC(C)=NN1CC)NC2=NC3=CC(C(N)=O)=CC(OC)=C3N2C/C=C/CN4C5=C(OCCCN(C)C)C=C(C(N)=O)C=C5N=C4NC(C6=CC(C)=NN6CC)=O.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (118.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1843 mL 5.9216 mL 11.8433 mL
5 mM 0.2369 mL 1.1843 mL 2.3687 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1843 mL 5.9216 mL 11.8433 mL 29.6082 mL
5 mM 0.2369 mL 1.1843 mL 2.3687 mL 5.9216 mL
10 mM 0.1184 mL 0.5922 mL 1.1843 mL 2.9608 mL
15 mM 0.0790 mL 0.3948 mL 0.7896 mL 1.9739 mL
20 mM 0.0592 mL 0.2961 mL 0.5922 mL 1.4804 mL
25 mM 0.0474 mL 0.2369 mL 0.4737 mL 1.1843 mL
30 mM 0.0395 mL 0.1974 mL 0.3948 mL 0.9869 mL
40 mM 0.0296 mL 0.1480 mL 0.2961 mL 0.7402 mL
50 mM 0.0237 mL 0.1184 mL 0.2369 mL 0.5922 mL
60 mM 0.0197 mL 0.0987 mL 0.1974 mL 0.4935 mL
80 mM 0.0148 mL 0.0740 mL 0.1480 mL 0.3701 mL
100 mM 0.0118 mL 0.0592 mL 0.1184 mL 0.2961 mL
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diABZI-4 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

diABZI-42138299-65-5diABZI4diABZI 4STINGIntegrinNF-κBSARS-CoVStimulator of Interferon GenesTMEM173MITAERISMPYSNuclear factor-κBNuclear factor-kappaBSARS coronavirusSTAT1IRF3TBK1Calu-3 human lung epithelial cellsMRC-5 human lung fibroblastsmurine bone marrow-derived macrophagesprimary human CD14+ monocytesACE2-A549 cellsInhibitorinhibitorinhibit

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