diABZI-4
Based on 1 publication(s) in Google Scholar
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.33%
- CAS No.: 2138299-65-5
- 화학식: C40H50ClN13O6
- 분자량:844.36
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) diABZI-4
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Biological Activity
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.
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Cell Line:MRC-5 human lung fibroblasts
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Concentration:50 nM, 500 nM
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Incubation Time:5 h, 24 h
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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.
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.
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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]
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Dosage:0.25-0.5 mg/kg
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Administration:i.n.; single dose; 3 hours pre-infection or 12 hours post-infection
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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).
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Animal Model:C57BL/6J mice (9−10 weeks old, female)[2]
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Dosage:0.1 mg/kg
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Administration:intranasal (i.n.); single administration
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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.
Chemical Information
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CAS No. 2138299-65-5
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Appearance Solid
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분자량 844.36
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화학식 C40H50ClN13O6
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Color Light yellow to light brown
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (288 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Humphries F, et al. A diamidobenzimidazole STING agonist protects against SARS-CoV-2 infection. Sci Immunol. 2021;6(59):eabi9002. [Content Brief]
[3]. Humphries F, et al. Targeting STING oligomerization with small-molecule inhibitors. Proc Natl Acad Sci U S A. 2023;120(33):e2305420120. [Content Brief]
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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