| Identification | Back Directory | [Name]
D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate) | [CAS]
2647441-36-7 | [Synonyms]
SHEN26
Obeldesivir
D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate)
RNA,SHEN26,viral load,ATV 006,ATV006,antiviral,SARS coronavirus,Vero E6 cells,podrugs,Inhibitor,ATV-006,SARS-CoV,inhibit | [Molecular Formula]
C16H19N5O5 | [MOL File]
2647441-36-7.mol | [Molecular Weight]
361.36 |
| Chemical Properties | Back Directory | [density ]
1.59±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 250 mg/mL (691.85 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.00±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Obeldesivir (ATV006) is a potent, orally active antiviral agent and ester proagents of GS-441524. Obeldesivir inhibits the replication of SARS-CoV-2 and its variants. Obeldesivir can be used for SARS-CoV-2 research[1]. | [in vivo]
Obeldesivir (5-25 mg/kg; p.o. and i.v.; Sprague Dawley rats) has favorable pharmacokinetic profiles in rats with high oral bioavailability (F %) of 81.5% and maximum blood concentration (Cmax) of 8.2 μM[1].
Obeldesivir (250-500 mg/kg; p.o.; daily, for 4 days; hACE2 knock-in and Ad5-hACE2 mice) has antiviral activity and inhibits SARS-CoV-2 replication in mouse models[1].
Obeldesivir (100-250 mg/kg; p.o.; daily, for 10 days) reduces lung damage and protects K18-hACE2 mice[1].
Obeldesivir (10-150 mg/kg; p.o.; daily, for 3 days) reduces virus titers and lung damage caused by Delta variant infection in K18-hACE2 mice[1]. | Animal Model: | Sprague Dawley rats[1] | | Dosage: | 5 and 25 mg/kg | | Administration: | Oral administration (25 mg/kg) and intravenous injection (5 mg/kg) | | Result: | 1.19|
| parameters | i.v. (5 mg/kg) | p.o. (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 |
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| Animal Model: | hACE2 knock-in and Ad5-hACE2 mice[1] | | Dosage: | 250 and 500 mg/kg | | Administration: | Oral administration; daily, for 4 days | | Result: | Inhibited gRNA and sgRNA, which is Biomarkers of coronavirus replication. Reduced the viral load and pathological damage of the lung. |
| Animal Model: | K18-hACE2 mice[1] | | Dosage: | 100 and 250 mg/kg | | Administration: | Oral administration; daily, for 10 days | | Result: | Reduced viral RNA and increased the survival rate of mice. Reduced evidence of lung pathology and the production of inflammatory cytokines and chemokines in the lung tissues. |
| Animal Model: | K18-hACE2 mice[1] | | Dosage: | 10, 30, 80 and 150 mg/kg | | Administration: | Oral administration; daily, for 3 days | | Result: | Reduced viral load in a dose-dependent manner and alleviated the symptoms in the lung. |
| [References]
[1] Cao L, et, al. The adenosine analog prodrug ATV006 is orally bioavailable and has preclinical efficacy against parental SARS-CoV-2 and variants. Sci Transl Med. 2022 May 17:eabm7621. DOI:10.1126/scitranslmed.abm7621 |
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