安瑞那韦 T6388

Product Introduction
Bioactivity


英文名: Amprenavir

描述: 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。

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.

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 13 mg/mL (25.7 mM)
Ethanol : 93 mg/mL (183.9 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: HIV | SARS coronavirus | Inhibitor | HIV Protease | KVX478 | VX478 | SARS-CoV | KVX 478 | inhibit | Amprenavir | VX 478 | Human immunodeficiency virus

相关产品: Z795161988 | Bemnifosbuvir hemisulfate | SARS-CoV-2-IN-61 | GNF-5 | Chloroquine phosphate | SARS-CoV-2-IN-51 | E 64c | SARS-CoV-2-IN-55 | Telaprevir | Azelastine

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | ReFRAME Related Library | Drug-induced Liver Injury (DILI) Compound Library | Anti-Metabolism Disease Compound Library | Human Metabolite Library | Inhibitor Library | EMA Approved Drug Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途