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| Targets |
ST-148 maleate targets the dengue virus (DENV) replication cycle. It acts as a host-targeting antiviral agent by disrupting the interaction between lipid droplets and the viral C (capsid) protein. Lipid droplets are cellular organelles that play a crucial role in the dengue virus replication cycle. The viral C protein associates with lipid droplets, and this interaction is essential for viral replication. By disrupting this interaction, ST-148 maleate inhibits viral replication. The compound's activity is independent of the viral serotype, as it targets a host factor, making it effective against all four DENV serotypes.
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| ln Vitro |
In vitro, ST-148 maleate is a potent inhibitor of all four serotypes of dengue virus. It demonstrates antiviral efficacy with low cell toxicity. The compound's mechanism of action involves altering the interaction between lipid droplets and the viral C protein, thereby inhibiting viral replication. Specific quantitative data such as IC50 values for viral inhibition have not been extensively reported in the available literature. The compound's low cell toxicity suggests a favorable safety profile for in vitro studies.
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| ln Vivo |
In vivo, ST-148 maleate is an orally active compound. It significantly reduces viremia. As a dengue virus inhibitor with oral activity, the compound is a promising candidate for in vivo studies. However, specific animal model studies, dosing regimens, and quantitative outcomes have not been extensively reported. The compound's ability to be administered orally is a significant advantage for potential therapeutic applications. Further in vivo studies would be required to characterize its efficacy, safety, and pharmacokinetic properties.
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| Enzyme Assay |
In vitro enzyme or receptor binding assay protocols are not directly applicable to ST-148 maleate, as its mechanism involves disrupting protein-protein or protein-lipid interactions. Its activity is assessed in cell-based antiviral assays.
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| Cell Assay |
A standard cell-based assay protocol for ST-148 maleate involves infecting susceptible cell lines (e.g., Vero or A549 cells) with dengue virus in the presence of varying concentrations of the compound. After incubation, viral replication is quantified by measuring viral RNA levels (by qRT-PCR), viral protein expression (by immunofluorescence or Western blot), or viral titers (by plaque assay). The compound's cytotoxicity is assessed in parallel using standard viability assays. The EC50 (half-maximal effective concentration) for viral inhibition and the CC50 (half-maximal cytotoxic concentration) are determined.
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| Animal Protocol |
In vivo animal experimental protocols for ST-148 maleate would typically involve using mouse models of dengue virus infection. A standard protocol would involve infecting immunocompromised or humanized mice with dengue virus and then administering the compound orally at doses determined from preliminary pharmacokinetic and tolerability studies. Endpoints would include viral load in blood and tissues (viremia), survival rates, and assessment of disease pathology. Appropriate controls would include vehicle-treated and untreated infected groups.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ST-148 maleate indicate that the compound is orally active. It has a molecular weight of 612.74. Specific PK parameters such as half-life, Cmax, AUC, bioavailability, volume of distribution, and clearance have not been extensively reported. The compound's metabolism, protein binding, and routes of elimination remain to be characterized. Further pharmacokinetic studies would be required to understand its absorption, distribution, metabolism, and excretion profile.
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| References | |
| Additional Infomation |
See also: ST-148 (Notes moved to).
ST-148 maleate is a research-grade compound that functions as a potent and orally active inhibitor of all four dengue virus serotypes. It disrupts the interaction between lipid droplets and the viral C protein. It has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action involves host-targeted antiviral activity, making it effective against a broad range of DENV serotypes. The compound is available exclusively for research purposes and is not intended for diagnostic, therapeutic, or human applications. |
| Molecular Formula |
C27H36N4O3S.C4H4O4
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|---|---|
| Molecular Weight |
612.7369
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| Exact Mass |
612.261
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| CAS # |
390803-40-4
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| PubChem CID |
11957682
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
43
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| Complexity |
854
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)C1=CC=CC2=C1C=CC=C2S(=O)(=O)NCCCCN3CCN(CC3)C4=CC=CC=C4OC.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
NMWGXMJVHMDGSA-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C27H36N4O3S.C4H4O4/c1-29(2)24-13-8-11-23-22(24)10-9-15-27(23)35(32,33)28-16-6-7-17-30-18-20-31(21-19-30)25-12-4-5-14-26(25)34-3;5-3(6)1-2-4(7)8/h4-5,8-15,28H,6-7,16-21H2,1-3H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
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| Chemical Name |
(Z)-but-2-enedioic acid;5-(dimethylamino)-N-[4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl]naphthalene-1-sulfonamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~58 mg/mL (~94.66 mM; with heating and sonication.)
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| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6320 mL | 8.1601 mL | 16.3201 mL | |
| 5 mM | 0.3264 mL | 1.6320 mL | 3.2640 mL | |
| 10 mM | 0.1632 mL | 0.8160 mL | 1.6320 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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