Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Amprenavir (KVX-478) 是一种 HIV 蛋白酶抑制剂,Ki 为0.6 nM。它也是 SARS-CoV 3CLpro 抑制剂,IC50为 1.09 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 153 | 现货 | ||
5 mg | ¥ 328 | 现货 | ||
10 mg | ¥ 525 | 现货 | ||
25 mg | ¥ 997 | 现货 | ||
50 mg | ¥ 1,590 | 现货 | ||
100 mg | ¥ 2,370 | 现货 | ||
500 mg | ¥ 5,620 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 368 | 现货 |
产品描述 | Amprenavir (KVX-478) is a synthetic derivative of hydroxyethylamine sulfonamide that selectively binds to and inhibits human immunodeficiency virus (HIV) protease. |
靶点活性 | HIV protease:14.6 ng/mL |
体外活性 | Amprenavir promotes the specific interactions between the nuclear receptor pregnane X receptor (PXR) and the coactivators SRC-1 and PBP. Amprenavir is docked into the high-resolution crystal structure of human PXR in complex with SR12813. Amprenavir occupies all four subpockets, and its hydroxyl group forms a hydrogen bond with Ser247, which is located in the connection region of PXR, to help to position the drug in the optimal orientation inside the receptor. Amprenavir forms direct contacts with one residue on αAF of the PXR activation function-2 (AF-2) surface, Phe429, which may stabilize the active AF-2 conformation of the receptor and contribute to the agonist activity of amprenavir on PXR. Amprenavir induces the expression of bona fide PXR target genes involved in phase I (CYP3A4), phase II (UGT1A1), and phase III (MDR1) metabolism in both HepaRG cells and LS180 cells. [1] |
体内活性 | Amprenavir increases atherogenic LDL cholesterol fractions in WT mice, but not in PXR?/? mice. Amprenavir stimulates expression of known PXR target genes, including CYP3A11, glutathione transferase A1, and MDR1a, in the intestine of WT mice but not in PXR?/? mice. Amprenavir-mediated PXR activation stimulates the expression of both LipF and LipA in the intestine of WT mice, but not in PXR?/? mice, indicating a possible role of intestinal PXR in mediating dietary lipid breakdown and absorption in mammals. [1] |
激酶实验 | PARP Enzyme Assay: The enzyme assay is conducted in buffer containing 50 mM Tris, pH 8.0, 1 mM dithiothreitol(DTT), and 4 mM MgCl2. PARP reactions contains 1.5 μM [3H]-NAD+ (1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Autoreactions utilizing SPA bead-based detection are carried out in 100 μL volumes in white 96-well plates. Reactions are initiated by adding 50 μL of 2X NAD+ substrate mixture to 50 μL of 2× enzyme mixture containing PARP and DNA. These reactions are terminated by the addition of 150 μL of 1.5 mM benzamide (~1 × 103-fold over its IC50). A 170 μL amount of the stopped reaction mixtures is transferred to streptavidin-coated Flash Plates, incubated for 1 hour, and counted using a TopCount microplate scintillation counter. Ki data are determined from inhibition curves at various substrate concentrations. |
别名 | 141W94, 安普那韦, Prozei, KVX-478, VX-478, 安瑞那韦 |
分子量 | 505.63 |
分子式 | C25H35N3O6S |
CAS No. | 161814-49-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 13 mg/mL (25.7 mM)
Ethanol: 93 mg/mL (183.9 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.9777 mL | 9.8887 mL | 19.7773 mL | 49.4433 mL |
5 mM | 0.3955 mL | 1.9777 mL | 3.9555 mL | 9.8887 mL | |
10 mM | 0.1978 mL | 0.9889 mL | 1.9777 mL | 4.9443 mL | |
20 mM | 0.0989 mL | 0.4944 mL | 0.9889 mL | 2.4722 mL | |
Ethanol | 50 mM | 0.0396 mL | 0.1978 mL | 0.3955 mL | 0.9889 mL |
100 mM | 0.0198 mL | 0.0989 mL | 0.1978 mL | 0.4944 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Amprenavir 161814-49-9 Microbiology/Virology Proteases/Proteasome SARS-CoV HIV Protease HIV SARS coronavirus 141W94 Inhibitor 安普那韦 Prozei KVX-478 KVX478 VX-478 VX478 KVX 478 inhibit VX 478 安瑞那韦 Human immunodeficiency virus inhibitor