| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
(S)-HN0037 targets the viral helicase-primase enzyme complex. This complex is essential for HSV DNA replication, as it unwinds the DNA helix and synthesizes RNA primers for DNA polymerase. By selectively inhibiting this complex, (S)-HN0037 blocks the replication of the viral genome, thereby preventing the production of new viral particles. The (S)-enantiomer is the active form of the inhibitor.
|
|---|---|
| ln Vitro |
(S)-HN0037 demonstrates potent in vitro antiviral activity by inhibiting the helicase-primase enzyme complex. This inhibition leads to a significant reduction in HSV DNA replication in cell-based assays. It is a selective inhibitor, meaning it targets the viral enzyme with high specificity, which translates to potent antiviral effects at low concentrations. The compound is orally active, indicating it can be effectively administered by this route to achieve therapeutic effects.
|
| ln Vivo |
(S)-HN0037 is an orally active helicase-primase inhibitor. While specific in vivo efficacy data is not detailed in the search results, the compound is described as a selective and orally active inhibitor that inhibits HSV replication. This suggests that it is effective in animal models of HSV infection when administered via the oral route.
|
| Enzyme Assay |
The inhibitory activity of (S)-HN0037 on the helicase-primase enzyme can be assessed using a cell-free helicase assay. Procedure: Recombinant HSV helicase-primase complex is incubated with varying concentrations of (S)-HN0037 (e.g., 0.001-1000 nM) in a reaction buffer containing ATP and a DNA substrate. After a 30-60 minute incubation at 37degC, the reaction is stopped, and DNA unwinding is quantified by measuring the amount of single-stranded DNA using a fluorescent dye or gel electrophoresis. The IC50 is calculated as the concentration required to inhibit 50% of the helicase activity.
|
| Cell Assay |
The in vitro antiviral activity can be assessed using a plaque reduction assay. Procedure: Vero cells are seeded in 6-well plates (5x10⁵ cells/well) and infected with HSV-1 or HSV-2 at a multiplicity of infection (MOI) of 0.01 PFU/cell. After 1 hour, the virus inoculum is removed, and cells are overlaid with culture medium containing varying concentrations of (S)-HN0037 (0.1-1000 nM). After 48-72 hours of incubation at 37degC, cells are fixed and stained with crystal violet. Plaques are counted, and the IC50 is determined as the concentration reducing plaque numbers by 50% compared to the virus-only control.
|
| Animal Protocol |
The in vivo efficacy of (S)-HN0037 can be evaluated in a mouse model of HSV infection. Procedure: Female BALB/c mice (6-8 weeks) are infected intranasally or intraperitoneally with a lethal dose of HSV-1 or HSV-2. Mice are randomized into groups (n=10 per group). (S)-HN0037 is formulated in a suitable vehicle (e.g., 0.5% methylcellulose) and administered orally at doses of 10, 30, and 100 mg/kg, once or twice daily for 7 days. Survival is monitored for up to 21 days. At the study endpoint, viral titers in target organs (e.g., brain, liver, or vaginal swabs) are determined by plaque assay on Vero cells.
|
| ADME/Pharmacokinetics |
(S)-HN0037 is an orally active compound. Specific PK parameters (t½, Cmax, AUC, bioavailability) are not provided in the search results. However, its designation as "orally active" indicates that it has sufficient oral bioavailability to achieve therapeutic plasma concentrations following oral administration. The compound is typically stored as a powder at -20degC for up to 3 years. The (S)-isomer is the active enantiomer, likely demonstrating superior PK properties compared to the racemic mixture.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for (S)-HN0037 is not provided in the search results. The compound is described as a research chemical for use only in laboratory settings, not for human therapeutic use. Standard safety precautions for handling research chemicals should be followed, including the use of gloves, lab coat, and safety goggles. Conduct all handling of the compound in a well-ventilated area or fume hood to avoid inhalation.
|
| References | |
| Additional Infomation |
(S)-HN0037 is a novel small molecule that functions as a selective and orally active inhibitor of the viral helicase-primase complex. It targets the helicase-primase enzyme complex, making it an effective anti-HSV agent by blocking viral DNA replication. This product is for research use only and is not an approved drug. The compound is available as a solid and is stored at -20degC.
|
| Molecular Formula |
C20H20N4O3S2
|
|---|---|
| Molecular Weight |
428.53
|
| CAS # |
2233566-78-2
|
| Appearance |
White to off-white solid powder
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
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
|
|---|---|
| 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 | 2.3336 mL | 11.6678 mL | 23.3356 mL | |
| 5 mM | 0.4667 mL | 2.3336 mL | 4.6671 mL | |
| 10 mM | 0.2334 mL | 1.1668 mL | 2.3336 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
