| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| Targets |
Obeldesivir targets the RNA-dependent viral RNA polymerase (RdRp), a highly conserved enzyme essential for viral replication. As a prodrug of GS-441524, it is converted to the active triphosphate form that competes with natural nucleotides for incorporation into viral RNA, causing chain termination and inhibiting viral replication. This mechanism is similar to other nucleoside analogs used against RNA viruses. It effectively inhibits SARS-CoV-2 and its variants.
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| ln Vitro |
Obeldesivir (0.001-100 μM; 48 h; Vero E6 cells) prevents both the pathogenic and real SARS-CoV-2 variants from replicating. Obeldesivir's effectiveness in blocking the replication of Delta and Omicron variants is improved overall by >4 and >12 times, respectively, with EC50 values of 0.349 μM and 0.106 μM[1].
In vitro, Obeldesivir effectively inhibits the replication of SARS-CoV-2 and its variants. As a nucleoside analog, it inhibits viral RNA-dependent RNA polymerase activity. The compound is an oral prodrug of GS-441524, which is the active parent nucleoside. These in vitro activities demonstrate its potential as an antiviral agent against SARS-CoV-2 and other RNA viruses. |
| ln Vivo |
The pharmacokinetic profiles of beldesivir (5–25 mg/kg; po and iv) in Sprague Dawley rats are favorable, with a high oral bioavailability (F%) of 81.5% and a maximum blood concentration (Cmax) of 8.2 μM[1]. Obeldesivir (250–500 mg/kg; po; daily, 4 days; Ad5-hACE2 and hACE2 knock-in mice) has antiviral activity and prevents the replication of SARS-CoV-2 in mouse models[1]. K18-hACE2 mice are protected and lung damage is decreased by kg; po; daily, for 10 days[1]. In K18-hACE2 mice, obeldesivir (10–150 mg/kg; po; daily, for 3 days) decreases virus titers and lung damage brought on by Delta variant infection[1].
In vivo, Obeldesivir is an orally active antiviral agent. As a prodrug of GS-441524, it is designed for oral administration with improved bioavailability compared to the parent compound. It has shown efficacy in preclinical models of SARS-CoV-2 infection. It is under investigation for the treatment of COVID-19 and other viral infections. |
| Enzyme Assay |
In vitro enzyme assays for Obeldesivir measure inhibition of viral RNA-dependent RNA polymerase (RdRp) activity. The compound is converted to its active triphosphate form, and its ability to inhibit RNA synthesis is assessed using purified RdRp enzyme and RNA templates. These assays characterize the compound's antiviral mechanism.
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| Cell Assay |
Cell-based assays for Obeldesivir are conducted in virus-infected cells. Cells are infected with SARS-CoV-2 or other viruses and treated with the compound at various concentrations. Viral replication is measured by plaque assay, qPCR, or viral protein expression. Cytotoxicity is assessed to determine the therapeutic index.
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| Animal Protocol |
Animal/Disease Models: Sprague Dawley rats[1]
Doses: 5 and 25 mg/kg Route of Administration: Oral administration (25 mg/kg) and intravenous (iv) injection (5 mg/kg) Experimental Results: 1.19 parameters iv (5 mg/kg) po (25 mg/kg) AUClast (μM·h) 5.6 22.8 T1/2 (h) 1.5 1.2 Tmax (h) 0.5 Cmax (μM) 8.7 8.2 F % 81.5 Animal/Disease Models: hACE2 knock- in and Ad5-hACE2 mice[1] Doses: 250 and 500 mg/kg Route of Administration: Oral administration; daily, for 4 days Experimental Results: Inhibited gRNA and sgRNA, which is Biomarkers of coronavirus replication. decreased the viral load and pathological damage of the lung. Animal/Disease Models: K18-hACE2 mice[1] Doses: 100 and 250 mg/kg Route of Administration: Oral administration; daily, for 10 days Experimental Results: decreased viral RNA and increased the survival rate of mice. decreased evidence of lung pathology and the production of inflammatory cytokines and chemokines in the lung tissues. Animal/Disease Models: K18-hACE2 mice[1] Doses: 10, 30, 80 and 150 mg/kg Route of Administration: Oral administration; daily, for 3 days Experimental Results: decreased viral load in a d In vivo animal experiments with Obeldesivir are conducted in mouse models of SARS-CoV-2 infection. The compound is administered orally, and viral load in tissues is measured. Efficacy is assessed by reduction in viral replication and improvement in survival and clinical parameters. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Obeldesivir include oral bioavailability as a prodrug of GS-441524. The compound is designed for oral administration with improved pharmacokinetic properties compared to the parent nucleoside. Specific PK parameters such as half-life, Cmax, and AUC have been reported in preclinical studies.
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| Toxicity/Toxicokinetics |
Safety and toxicology data for Obeldesivir are being evaluated in preclinical and clinical studies. As a nucleoside analog, potential toxicities include effects on host cell DNA and RNA synthesis. The compound is for research use and is not approved for clinical use without appropriate regulatory approval.
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| References | |
| Additional Infomation |
Obeldesivir has CAS number 2647441-36-7, molecular formula C16H19N5O5, and molecular weight 361.35【35†30】. Synonyms: GS-5245, ATV-006【35†23】. It is an oral prodrug of GS-441524 targeting viral RNA polymerase【35†5-L6】. It inhibits SARS-CoV-2 replication【35†24】. It is an investigational antiviral drug【35†35-L37】. Not for clinical use without approval; for research purposes only.
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| Molecular Formula |
C16H19N5O5
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|---|---|
| Molecular Weight |
361.35
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| Exact Mass |
361.138
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| CAS # |
2647441-36-7
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| PubChem CID |
162513664
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| Appearance |
White to off-white solid powder
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| LogP |
-0.3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
595
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C([C@]1(C2=CC=C3C(=NC=NN23)N)[C@@H]([C@H](O)[C@@H](COC(=O)C(C)C)O1)O)#N
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| InChi Key |
YIHPGVCWGSURHO-VSBTWAGUSA-N
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| InChi Code |
InChI=1S/C16H19N5O5/c1-8(2)15(24)25-5-10-12(22)13(23)16(6-17,26-10)11-4-3-9-14(18)19-7-20-21(9)11/h3-4,7-8,10,12-13,22-23H,5H2,1-2H3,(H2,18,19,20)/t10-,12-,13-,16+/m1/s1
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| Chemical Name |
[(2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxyoxolan-2-yl]methyl 2-methylpropanoate
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| Synonyms |
Obeldesivir GS-5245 ATV-006 SHEN-26GS5245 ATV006 SHEN26
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~250 mg/mL (~691.85 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 | 2.7674 mL | 13.8370 mL | 27.6740 mL | |
| 5 mM | 0.5535 mL | 2.7674 mL | 5.5348 mL | |
| 10 mM | 0.2767 mL | 1.3837 mL | 2.7674 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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