Obeldesivir ATV006|cas:2647441-36-7|西域试剂

Obeldesivir ATV006,99.41%

产品编号：Bellancom-145994| CAS NO：2647441-36-7| 分子式：C₁₆H₁₉N₅O₅| 分子量：361.35

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货号	价格	库存与货期
Bellancom-145994	￥3000.00	杭州北京（现货）
Bellancom-145994	￥4800.00	杭州北京（现货）
Bellancom-145994	￥9500.00	杭州北京（现货）
Bellancom-145994	￥14500.00	杭州北京（现货）

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Obeldesivir ATV006

产品介绍

Obeldesivir (ATV006) 是一种口服有效的抗病毒剂和 GS-441524 酯类前体。 Obeldesivir 能有效抑制 SARS-CoV-2 及其变体的复制。Obeldesivir 可用于SARS-CoV-2 研究。

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 (C_max) 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

parameters	i.v. (5 mg/kg)	p.o. (25 mg/kg)
AUC_last (μM·h)	5.6	22.8
T_1/2 (h)	1.5	1.2
T_max (h)		0.5
C_max (μM)	8.7	8.2
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

parameters	i.v. (5 mg/kg)	p.o. (25 mg/kg)
AUC_last (μM·h)	5.6	22.8
T_1/2 (h)	1.5	1.2
T_max (h)		0.5
C_max (μM)	8.7	8.2
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (691.85 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献