产品
编 号：F741698
分子式：C16H19N5O5
分子量：361.35
分子式：C16H19N5O5
分子量：361.35
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2647441-36-7
产品详情
生物活性：
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.
体内研究：
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.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.Obeldesivir (100-250 mg/kg; p.o.; daily, for 10 days) reduces lung damage and protects K18-hACE2 mice.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.Animal Model:Sprague Dawley rats
Dosage:5 and 25 mg/kg
Administration:Oral administration (25 mg/kg) and intravenous injection (5 mg/kg)
Result:1.19 parametersi.v. (5 mg/kg)p.o. (25 mg/kg)
AUClast (μM·h)5.622.8
T1/2 (h)1.51.2
Tmax (h)0.5
Cmax (μM)8.78.2
F %81.5
Animal Model:hACE2 knock-in and Ad5-hACE2 mice
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
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
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.
体外研究：
Obeldesivir (0.001-100 μM; 48 h; Vero E6 cells) inhibits the replication of authentic SARS-CoV-2 and its variants of concern. Obeldesivir has an overall >4-fold and >12-fold potency improvement in inhibiting the replication of Delta and Omicron variants, with EC50 values of 0.349 μM and 0.106 μM, respectively.
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.
体内研究：
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.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.Obeldesivir (100-250 mg/kg; p.o.; daily, for 10 days) reduces lung damage and protects K18-hACE2 mice.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.Animal Model:Sprague Dawley rats
Dosage:5 and 25 mg/kg
Administration:Oral administration (25 mg/kg) and intravenous injection (5 mg/kg)
Result:1.19 parametersi.v. (5 mg/kg)p.o. (25 mg/kg)
AUClast (μM·h)5.622.8
T1/2 (h)1.51.2
Tmax (h)0.5
Cmax (μM)8.78.2
F %81.5
Animal Model:hACE2 knock-in and Ad5-hACE2 mice
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
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
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.
体外研究：
Obeldesivir (0.001-100 μM; 48 h; Vero E6 cells) inhibits the replication of authentic SARS-CoV-2 and its variants of concern. Obeldesivir has an overall >4-fold and >12-fold potency improvement in inhibiting the replication of Delta and Omicron variants, with EC50 values of 0.349 μM and 0.106 μM, respectively.
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