AVG-233|cas:2151937-80-1|西域试剂

AVG-233,98.87%

产品编号：Bellancom-122587| CAS NO：2151937-80-1| 分子式：C₂₆H₂₂ClN₅O₃| 分子量：487.94

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-122587	￥4000.00	杭州北京（现货）
Bellancom-122587	￥6800.00	杭州北京（现货）
Bellancom-122587	￥13500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

AVG-233

产品介绍

AVG-233 是一种口服有效的 RNA 依赖性 RNA 聚合酶 (RdRp) 抑制剂。AVG-233 阻止启动子上的病毒聚合酶复合物的启动。AVG-233 结合位点存在于 L_1-1749 片段中。AVG-233 对 RSV 毒株和临床分离株均具有纳摩尔活性 (EC₅₀=0.14-0.31 μM)。AVG-233 可用于呼吸道合胞病毒 (RSV) 研究。

生物活性

AVG-233 is a potent, orally active RNA dependent RNA polymerase (RdRp) inhibitor. AVG-233 prevents initiation of the viral polymerase complex at the promoter. AVG-233 binding site is present in the L_1-1749 fragment. AVG-233 has nanomolar activity against both RSV strains and clinical RSV isolates (EC₅₀=0.14-0.31 μM). AVG-233 can be used for research of respiratory syncytial virus (RSV).

体外研究

AVG-233 (1-100 μM) blocks 3´RNA extension elongation but does not interfere with 3´RNA extension by up to three nucleotides after de novo initiation from the promoter or back-priming.
AVG-233 (20 μM) reduces virus yield of RSV A2-L19F (EC₅₀=0.31 μM), RSV strain 2-20 (EC₅₀=0.14 μM) and RSV clinical isolate 718 (EC₅₀=0.2 μM) .
AVG-233 (1.25-40 μM; 0-300 s) suppresses RNA synthesis by the L1-1749 fragment in a dose-dependent manner with an IC₅₀ value of 13.7 μM. AVG-233 bounds L and the L_1-1749 fragment with similar affinities (dissociation constants (KD’s) are 38.3 μM and 53.1 μM, respectively).

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

体内研究

AVG-233 (50-100 mg/kg; i.g.; once) decreases lung viral load in the RSV mouse model.
AVG-233 (2-20 mg/kg; i.v. and p.o.; once; male CD-1 mice) has good orally bioavailable and the maximum plasma concentration about 2 μM.

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

Animal Model:	Female Balb/cJ mice with recRSV-mKate xenograft
Dosage:	50 and 100 mg/kg
Administration:	Oral gavage; once
Result:	Reduced in lung viral load of 0.89 log₁₀ TCID₅₀ (median tissue culture infectious dose)/mL.

Animal Model:

Male CD-1 mice (27-29 g)

Dosage:

2 mg/kg (i.v.) and 20 mg/kg (p.o.)

Administration:

Intravenous injection and oral administration; once, obtains blood samples at pre-dose and 0.083, 0.25, 0.5, 1, 2, 4, 8, and 24 h post-dosing

Result:

1.19

Route	Dose	T_max	C_max	AUC_0-∞	CL/F	T_1/2	Bioavailability
	mg/kg	h	nmol/ml	h×nmol/ml	liters/h/kg	h	%
Oral	20	1	2.17	5.95	6.98	5.28	33.8

体内研究

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

Animal Model:	Female Balb/cJ mice with recRSV-mKate xenograft
Dosage:	50 and 100 mg/kg
Administration:	Oral gavage; once
Result:	Reduced in lung viral load of 0.89 log₁₀ TCID₅₀ (median tissue culture infectious dose)/mL.

Animal Model:

Male CD-1 mice (27-29 g)

Dosage:

2 mg/kg (i.v.) and 20 mg/kg (p.o.)

Administration:

Intravenous injection and oral administration; once, obtains blood samples at pre-dose and 0.083, 0.25, 0.5, 1, 2, 4, 8, and 24 h post-dosing

Result:

1.19

Route	Dose	T_max	C_max	AUC_0-∞	CL/F	T_1/2	Bioavailability
	mg/kg	h	nmol/ml	h×nmol/ml	liters/h/kg	h	%
Oral	20	1	2.17	5.95	6.98	5.28	33.8

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (102.47 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0494 mL	10.2472 mL	20.4943 mL
5 mM	0.4099 mL	2.0494 mL	4.0989 mL
10 mM	0.2049 mL	1.0247 mL	2.0494 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 (sealed storage, away from moisture and 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, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

参考文献