VGD020 (0.01-10 μM; 4-5 days) effectively inhibited the replication of DENV2 in Vero cells and achieved complete antiviral activity at micromolar concentrations [1]. VGD020 (0.01-100 μM; 4-5 days) showed low cytotoxicity to Vero cells, and even at concentrations as high as 100 μM, its effect on cell viability was minimal [1]. VGD020 (0.01-10 μM; 4-5 days) effectively inhibited the replication of DENV2 in Huh7 cells and achieved complete antiviral activity at micromolar concentrations [1]. VGD020 (0.02-2 μM; 48 hours) inhibited the expression of viral E protein in Huh7 cells infected with dengue virus type 2 (DENV2), and complete inhibition was achieved after 48 hours of treatment at a concentration of 0.4 μM [1]. VGD020 (2 μM; 72 h) effectively inhibited the expression of viral E protein in dengue virus type 2 (DENV2) infected Huh7 cells [1]. VGD020 (1 μM; 0-24 h) exerted an antiviral effect on DENV2 after the virus entered Vero cells, and maintained full activity even when added 8 h after infection [1]. VGD020 (0.4-10 μM; 18 h) inhibited the expression of DENV2 prM and E proteins in transiently transfected HEK293T cells in a concentration-dependent manner, and its efficacy was consistent with its antiviral activity [1]. Even at a concentration as high as 10 μM, VGD020 (0.4-10 μM; 18 h) did not inhibit the expression of DENV2 NS1 protein in transiently transfected HEK293T cells [1]. VGD020 (0.4-10 μM; 18 h) selectively inhibited the expression of DENV2 prM protein in transiently transfected HEK293T cells, but did not inhibit the expression of E protein [1]. VGD020 (0.15-15 μM) selectively inhibited Sec61-mediated cotranslational translocation of DENV2 prM protein to the endoplasmic reticulum lumen in cell-free experiments without affecting protein translation [1]. VGD020 (0.15-15 μM) did not inhibit Sec61-mediated cotranslational translocation of truncated DENV2 E protein to the endoplasmic reticulum lumen in cell-free experiments [1]. VGD020 (0.4-10 μM; 18 h) induced inhibition of DENV2 polyprotein transport, leading to proteasome degradation of its precursor protein; in CHO-K1 cells, MG132 co-treatment could partially reverse this effect [1]. VGD020 (0.01-10 μM; 18 h) effectively inhibited the expression of 14C-prM62-VSV-G chimeric protein in HEK293T cells, with an IC50 of 308 nM [1]. Even at concentrations as high as 10 μM, VGD020 (0.01-10 μM; 18 h) did not inhibit the expression of M21-E62-VSV-G or E23-NS162-VSV-G chimeric proteins in HEK293T cells [1]. VGD020 (0.01-10 μM; 18 h) effectively inhibited the expression of chimeric proteins containing the DENV2 C14 signal peptide sequence (a major determinant of VGD020 sensitivity) in HEK293T cells, with an IC50 of 41 nM [1]. VGD020 (0.01-10 μM; 18 hours) effectively inhibited the expression of chimeric proteins containing the C14 signal peptide sequence of various flaviviruses (DENV1, DENV3, DENV4, ZIKV) in HEK293T cells, with its IC50 value remaining stable at approximately 100 nM [1]. VGD020 (18 hours) downregulated the expression of sortilin in HEK293T cells in a dose-dependent manner, with an IC50 value of 0.5 μM [2]. VGD020 (24 hours) effectively downregulated CD4 expression in CHO CD4-YFP cells, with an IC50 of 46 nM [3].

Western Blot Analysis [1]
Cell Types: DENV2-infected Huh7 cells
Tested Concentrations: 0.02, 0.08, 0.4, and 2 μM
Incubation Duration: 48 hours
Experimental Results: 0.4 μM completely inhibited viral E protein expression in cells. Compared with the untreated infected control group, viral E protein expression was partially inhibited at lower concentrations.

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Western Blot Analysis [1]
Cell Types: Transiently transfected HEK293T cells (plasmid encoding DENV2 C14-prM-E)
Tested Concentrations: 0.4, 2, and 10 μM
Incubation Duration: 18 hours
Experimental Results: The expression of both prM and E proteins was inhibited in a concentration-dependent manner. Significant inhibition was achieved at all tested concentrations compared to the untreated transfected control group.

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Western Blot Analysis [1]
Cell Types: Transiently transfected HEK293T cells (plasmid encoding DENV2 E23-NS1-V5)
Tested Concentrations: 0.4, 2, and 10 μM
Incubation Duration: 18 hours
Experimental Results: At concentrations up to 10 μM, there was no inhibitory effect on NS1 protein expression. NS1 expression levels were comparable to those in the untreated transfected control group.

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Western Blot Analysis [1]
Cell Types: Transiently transfected HEK293T cells (transfected plasmid encoding DENV2 M21-E or C14-prM)
Tested Concentrations: 0.4, 2, and 10 μM
Incubation Duration: 18 hours
Experimental Results: Concentration-dependent inhibition of prM protein expression was observed, with significant inhibition at 2 and 10 μM concentrations. E protein expression was not inhibited at any of the tested concentrations.

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Western Blot Analysis [1]
Cell Types: Transiently transfected CHO-K1 cells (plasmid encoding DENV2 C14-prM-E_V5/FLAG/MYC)
Tested Concentrations: 0.4, 2, and 10 μM (alone or in combination with 200 nM MG132)
Incubation Duration: 18 hours
Experimental Results: When used in combination with MG132, a small amount of uncut prM-E polyprotein precursor (75 kDa) was detected, while this precursor was not detected in samples treated with VGD020 alone or in untreated samples. The precursor produced in the combined treatment samples was non-glycosylated.

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[1]. Sec61 translocon inhibitor flavitransin blocks selectively dengue virus polyprotein insertion in the ER with pan-orthoflavivirus antiviral potency. Cell Rep. 2025 Dec 23;44(12):116642.

[2]. Reduction of Progranulin-Induced Breast Cancer Stem Cell Propagation by Sortilin-Targeting Cyclotriazadisulfonamide (CADA) Compounds. J Med Chem. 2021;64(17):12865-12876.

[3]. Unsymmetrical cyclotriazadisulfonamide (CADA) compounds as human CD4 receptor down-modulating agents. J Med Chem. 2011;54(16):5712-5721.

C31H45N3O5S2

603.84

1322645-32-8

Typically exists as solids at room temperature

O=S(C1=CC=C(C=C1)OC)(N2CC(CN(S(=O)(C3=CC=C(C)C=C3)=O)CCCN(CC4CCCCC4)CCC2)=C)=O

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)