规格

价格

库存

数量

1 mg

¥ 388

现货

5 mg

¥ 1,320

现货

10 mg

¥ 2,120

现货

25 mg

¥ 3,570

现货

50 mg

¥ 4,970

现货

100 mg

¥ 6,870

现货

200 mg

¥ 9,450

现货

1 mL x 10 mM (in DMSO)

¥ 1,680

现货

生物活性

产品描述	Asunaprevir (BMS-650032) is an effective hepatitis C virus (HCV) NS3 protease inhibitor.
靶点活性	HCV 1a H77:0.7 nM, 5a (SA13):1.7 nM, 6a (HK-6A):0.9 nM, 4a (ED43):1.6 nM, 1b J4L6S:0.3 nM
体外活性	Asunaprevir抑制基因型1a（H77株）和基因型1b（J4L6S株）的NS3蛋白酶活性，其IC50分别为0.7和0.3 nM。针对编码NS3蛋白酶领域的基因型1a、1b和4a的复制子，ASV的EC50值在1.2到4.0 nM之间[2]。在以10倍和30倍EC50值（分别为50或150 nM最终浓度）的Asunaprevir浓度下，维持复制子细胞的选择性压力。对于基因型1b的抗性选择，以10倍或30倍EC50值（分别为30或90 nM最终浓度）的Asunaprevir浓度维持复制子细胞[3]。单次或多次给药，每日两次，剂量从200到600 mg的Asunaprevir通常被患者良好耐受，能在慢性感染基因型1 HCV的受试者中快速且大幅降低HCV RNA水平[4]。
体内活性	Asunaprevir（3-15 mg/kg，p.o.）在多种动物种类中表现出肝脏靶向性质，肝脏至血浆比例在不同物种间从40至359倍不等。在给药后24小时，所有测试物种的肝脏暴露度普遍达到或超过抑制剂EC50（针对HCV基因型1复制子）的110倍以上[2]。
细胞实验	Cytotoxicity is determined by incubating cells (3,000 to 10,000 cells/well) with serially diluted test compounds or DMSO for 5 days (MT-2 cells) or 4 days (all other cell types). Cell viability is quantitated using an MTS assay for MT-2 or a Cell-Titer Blue reagent assay for HEK-293, HuH-7, HepG2, and MRC5 cells, and 50% cytotoxic concentrations (CC50s) are calculated.
动物实验	Mice (n=9 per group; overnight fast) receive Asunaprevir (ASV) by oral gavage (5 mg/kg; a vehicle of PEG-400-ethanol, 9:1). Blood samples (-0.2 mL) are obtained by retro-orbital bleeding at 0.25, 0.5, 1, 3, 6, 8, and 24 h after dosing. Within each group, three animals are bled at 0.25, 3, and 24 h, three at 0.5 and 6 h, and three at 1 and 8 h, resulting in a composite pharmacokinetic profile. Livers and brains are also removed from mice at the terminal sampling points. Rats (n=3 per group; overnight fast) receive ASV (amorphous free acid) by oral gavage (3, 5, 10, and 15 mg/kg) in PEG-400-ethanol (9:1). Serial blood samples (-0.3 mL) are obtained from the jugular vein predosing (0 h) and at 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 24, and 48 h post dosing. To assess tissue exposure, rats are orally administered ASV (5 or 15 mg/kg, same vehicle as above), and blood, liver, and heart samples from two rats/group are obtained at 0.17, 0.5, 1, 2, 4, 6, 8, 24, 48, and 72 h after dosing.
别名	阿那匹韦, BMS-650032

化学信息

分子量	748.29
分子式	C₃₅H₄₆ClN₅O₉S
CAS No.	630420-16-5
Smiles	COc1cnc(O[C@H]2C[C@H](N(C2)C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)(C)C)C(=O)N[C@@]2(C[C@H]2C=C)C(=O)NS(=O)(=O)C2CC2)c2cc(Cl)ccc12
密度	1.37 g/cm3

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

H2O: Insoluble

Ethanol: 20 mg/mL (26.73 mM), Sonication is recommended.

DMSO: 250 mg/mL (334.1 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (2.67 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.3364 mL	6.6819 mL	13.3638 mL	66.8190 mL
5 mM	0.2673 mL	1.3364 mL	2.6728 mL	13.3638 mL
10 mM	0.1336 mL	0.6682 mL	1.3364 mL	6.6819 mL
20 mM	0.0668 mL	0.3341 mL	0.6682 mL	3.3410 mL