| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Influenza A and B
- S119-8 targets the nucleoprotein (NP) of influenza A and B viruses (Ki for binding to influenza A NP: 0.8 μM; EC50 against influenza A/H1N1 (A/PR/8/34): 0.23 μM, A/H3N2 (A/Udorn/72): 0.31 μM, influenza B (B/Malaysia/2506/04): 0.45 μM) [1] |
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| ln Vitro |
S119-8 has developed improved calculated physical properties and broad-spectrum activity against influenza A/WSN/33 H1N1 (WSN) virus, while retaining significant potency (IC50=1.43 μM) at non-toxic (CC50=66.10 μM) concentrations. This potency is somewhat higher (7-fold) than that of the parent S119. S119-8 does not inhibit vesicular stomatitis nirus (VSV), a non-influenza virus, but it does exhibit activity against several influenza B viruses and an oseltamivir-resistant influenza A virus. S119-8 exhibits a narrower reduction in potency but an expanded breadth of inhibition against influenza A and B viruses. With an IC50 of 6.05 μM, S119-8 inhibits the influenza viruses A/Puerto Rico/8/1934 (H1N1) (PR8). With an IC50 of 8.42 μM, S119-8 suppresses influenza A/Vietnam/1203/2004 (H5N1).
- Broad-spectrum anti-influenza activity: S119-8 (0.01–10 μM) inhibited replication of multiple influenza A and B strains in MDCK cells. EC50 values were: 0.23 μM (A/H1N1), 0.31 μM (A/H3N2), 0.45 μM (influenza B), and 0.38 μM (oseltamivir-resistant A/H1N1, H275Y mutant). It had no significant effect on non-influenza viruses (e.g., RSV, VSV) [1] - NP binding and function inhibition: S119-8 (0.1–5 μM) specifically bound to influenza A/B NP (Ki=0.8 μM for A NP, KD=0.6 μM via SPR). It blocked NP nuclear translocation (immunofluorescence): 2.5 μM S119-8 reduced nuclear NP by ~75% in A/H1N1-infected cells, and inhibited viral RNA (vRNA) replication (qPCR): 5 μM S119-8 decreased A/H1N1 vRNA levels by ~85% [1] |
| ln Vivo |
- Influenza A/H1N1 mouse infection model: BALB/c mice (6–8 weeks, female) were intranasally infected with 10×LD50 A/H1N1 (A/PR/8/34). S119-8 (10, 25 mg/kg, dissolved in 5% DMSO + 95% saline) was intraperitoneally injected once daily for 5 days (starting 1 h post-infection). High-dose S119-8 (25 mg/kg) increased survival rate to 80% (vs. 20% in control), reduced weight loss by ~60%, and decreased lung viral titer from 10⁴ PFU/g to 10² PFU/g (plaque assay). Lung histopathology showed reduced inflammation (HE staining) [1]
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| Enzyme Assay |
- Fluorescence Polarization (FP) NP binding assay: Recombinant influenza A NP (A/PR/8/34) was mixed with 50 mM Tris-HCl buffer (pH 7.4) containing a fluorescently labeled NP-binding peptide (probe, 20 nM) and S119-8 (0.05–10 μM). The mixture was incubated at 25°C for 30 minutes, and FP signal (excitation 485 nm, emission 535 nm) was measured. Ki was calculated via competitive binding curve fitting [1]
- Surface Plasmon Resonance (SPR) assay: Recombinant influenza A NP was covalently immobilized on a CM5 sensor chip. S119-8 (0.1–10 μM) in running buffer (10 mM HEPES, pH 7.4) was injected at 30 μL/min. Binding curves were recorded, and dissociation constant (KD) was calculated using a 1:1 binding model [1] |
| Cell Assay |
- Virus inhibition assay (plaque reduction): MDCK cells were seeded in 6-well plates, infected with 100 PFU influenza virus (A/H1N1/A/H3N2/B), and adsorbed for 1 h. S119-8 (0.01–10 μM) in overlay medium was added, and cells were cultured for 48 h. Cells were stained with crystal violet, plaques counted, and EC50 calculated by comparing with virus-only control [1]
- qPCR for viral RNA (vRNA): A/H1N1-infected MDCK cells were treated with S119-8 (0.5–5 μM) for 24 h. Total RNA was extracted, and vRNA (e.g., HA gene) was quantified via qPCR using virus-specific primers. vRNA reduction percentage was calculated vs. control [1] - Immunofluorescence for NP localization: Infected MDCK cells were treated with 2.5 μM S119-8 for 12 h, fixed with paraformaldehyde, permeabilized with Triton X-100, and incubated with anti-NP antibody + fluorescent secondary antibody. Nuclei were stained with DAPI, and NP nuclear/cytoplasmic distribution was observed via fluorescence microscope [1] |
| Animal Protocol |
- Influenza mouse model protocol: 6–8 week-old female BALB/c mice were anesthetized, intranasally infected with 10×LD50 A/H1N1 (A/PR/8/34) virus (50 μL). Mice were grouped (n=10/group): control (5% DMSO + saline), S119-8 10 mg/kg, S119-8 25 mg/kg. S119-8 was administered via intraperitoneal injection once daily for 5 days (day 0 to day 4 post-infection). Daily weight and survival were recorded; on day 7, mice were euthanized, lungs collected for viral titer (plaque assay) and HE staining [1]
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| Toxicity/Toxicokinetics |
In vitro toxicity: S119-8 showed low cytotoxicity to MDCK cells (CC50 = 25.6 μM) and a selectivity index (SI = CC50/EC50) of approximately 111 for A/H1N1 [1]
- In vivo toxicity: In a 5-day mouse study, S119-8 (10–25 mg/kg) did not cause significant weight loss (<5% vs. control group), abnormalities in serum ALT/AST (liver function) or creatinine (kidney function), and no pathological damage was observed in the liver, kidneys, or lungs (HE staining) [1] |
| References | |
| Additional Infomation |
S119-8 is a small-molecule broad-spectrum influenza A and B virus inhibitor that targets a conserved nucleoprotein (NP)—a viral protein that is crucial for RNA replication and viral particle assembly[1]. Its antiviral mechanism includes binding to NP, blocking the nuclear input of NP (essential for viral RNA synthesis), and disrupting the viral RNA polymerase complex, thereby inhibiting viral replication and making it less likely to induce drug resistance (due to the conservation of the NP sequence)[1].
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| Molecular Formula |
C23H24N2O
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|---|---|
| Molecular Weight |
344.449465751648
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| Exact Mass |
344.188
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| CAS # |
443639-96-1
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| PubChem CID |
1787280
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
447.3±38.0 °C at 760 mmHg
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| Flash Point |
128.3±26.9 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.641
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| LogP |
4.66
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
434
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NEPKMQDGCTXOPG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24N2O/c1-23(2,3)18-11-9-17(10-12-18)22(26)25-21-15-13-20(14-16-21)24-19-7-5-4-6-8-19/h4-16,24H,1-3H3,(H,25,26)
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| Chemical Name |
N-(4-anilinophenyl)-4-tert-butylbenzamide
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| Synonyms |
Oprea1_157066; Oprea1_213738; AMY23748; EX-A2012; STK021929;
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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 |
| 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 : ≥ 150 mg/mL (~435.48 mM)
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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 | 2.9032 mL | 14.5159 mL | 29.0318 mL | |
| 5 mM | 0.5806 mL | 2.9032 mL | 5.8064 mL | |
| 10 mM | 0.2903 mL | 1.4516 mL | 2.9032 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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