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| Targets |
SHEN26 targets the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, the enzyme responsible for viral RNA replication. It inhibits RdRp with an IC50 of 1.36 μM. As a 5'-cyclohexanecarboxylate derivative of GS-441524, it acts as a nucleoside analog that is incorporated into viral RNA, causing chain termination and inhibition of viral nucleic acid synthesis. It is used for research on COVID-19.
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| ln Vitro |
SHEN26 (ATY014) has IC50 values of 1.12 μM and 0.35 μM for the beta and delta variants, respectively[1].
In vitro studies demonstrate that SHEN26 is a potent inhibitor of SARS-CoV-2 RdRp with an IC50 of 1.36 μM. As a 5'-cyclohexanecarboxylate derivative of GS-441524, it functions as a nucleoside analog that is incorporated into viral RNA, leading to chain termination and inhibition of viral replication. The compound shows antiviral activity against SARS-CoV-2 in cell-based systems. Detailed cellular assay data, including EC50 values in infected cell lines, are not extensively documented in the available literature. |
| ln Vivo |
In vivo activity of SHEN26 is attributed to its oral bioavailability and potent RdRp inhibition. As an orally active compound, it is designed for convenient administration in research settings. The compound inhibits viral nucleic acid synthesis, achieving antiviral effects. It has been investigated for its potential in treating COVID-19. Detailed in vivo efficacy data from animal models, including dose-response relationships and viral load reduction, are not extensively documented in the available literature.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for SHEN26 involves measuring its inhibitory activity against SARS-CoV-2 RNA-dependent RNA polymerase (RdRp). The assay typically uses purified recombinant RdRp enzyme incubated with the compound at varying concentrations, along with RNA template, primers, and nucleotide substrates. Polymerase activity is measured by quantifying RNA synthesis using methods such as radiometric detection, fluorescence, or gel-based assays. The IC50 value of 1.36 μM is determined by plotting percentage inhibition against compound concentration.
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| Cell Assay |
In vitro cell-based assays for SHEN26 are conducted using SARS-CoV-2-infected cell lines such as Vero E6 or Calu-3 cells. Cells are treated with the compound at various concentrations, and antiviral activity is assessed by measuring viral RNA levels using quantitative RT-PCR, viral titers by plaque assay, or cytopathic effect reduction. Cytotoxicity is evaluated using standard cell viability assays to determine the selectivity index. The compound's ability to inhibit viral replication is compared to appropriate positive controls.
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| Animal Protocol |
In vivo animal studies for SHEN26 are typically conducted using mouse models of SARS-CoV-2 infection, such as transgenic hACE2 mice or adapted virus models. Animals are administered the compound orally at various doses, and antiviral efficacy is evaluated by measuring lung viral titers, viral RNA levels, and histopathological changes. Pharmacokinetic parameters are determined from plasma samples. The compound's oral activity is evaluated by comparing efficacy following oral administration.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SHEN26 include oral activity, indicating good oral bioavailability. The compound is a 5'-cyclohexanecarboxylate derivative of GS-441524. It has a molecular formula of C19H23N5O5 and a molecular weight consistent with this structure. Detailed pharmacokinetic parameters such as half-life, Cmax, and tissue distribution are not extensively documented in the available literature. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
Toxicity information for SHEN26 is limited in the available literature. As a research-use compound, standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. Cytotoxicity should be evaluated in cell-based assays to determine the therapeutic window. No detailed toxicity data are available from the search results.
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| References | |
| Additional Infomation |
SHEN26 (ATV014) is a potent and orally active RdRp inhibitor with an IC50 of 1.36 μM against SARS-CoV-2. It is a 5'-cyclohexanecarboxylate derivative of GS-441524. SHEN26 inhibits viral nucleic acid synthesis, achieving antiviral effects. It is used for research on COVID-19. The compound is intended for research use only and is not for human therapeutic applications.
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| Molecular Formula |
C19H23N5O5
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| Molecular Weight |
401.416424036026
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| CAS # |
2691076-98-7
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| Appearance |
White to off-white solid powder
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| SMILES |
O1[C@H](COC(C2CCCCC2)=O)[C@H]([C@H]([C@]1(C#N)C1=CC=C2C(N)=NC=NN12)O)O
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| Synonyms |
SHEN26; ATY014; SHEN-26; ATY-014; SHEN 26; ATY 014; 2691076-98-7; ((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methyl cyclohexanecarboxylate; orb2565297; SCHEMBL24312623; PD201469;
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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) |
Typically soluble in DMSO (e.g. 10 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 | 2.4912 mL | 12.4558 mL | 24.9116 mL | |
| 5 mM | 0.4982 mL | 2.4912 mL | 4.9823 mL | |
| 10 mM | 0.2491 mL | 1.2456 mL | 2.4912 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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