富马酸替诺福韦酯, 人体免疫缺陷病毒 1 型逆转录酶抑制剂

CAS: 202138-50-9 货号: T408656 分子式: C23H34N5O14P 分子量: 635.51 EC号: 687-766-5 PubChem CID: 6398764
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
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规格
库存
价格
数量
1ml
T408656-1ml
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¥398.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。

概述

Tenofovir Disoproxil Fumarate 是核苷酸逆转录酶抑制剂 (nucleotide reverse transcriptase inhibitor),有潜力用于艾滋病和慢性乙型肝炎的研究。

Information

Tenofovir (GS 1278) Disoproxil Fumarate Tenofovir Disoproxil Fumarate (GS-1278, Tenofovir DF) belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-tri
In vitro

Tenofovir is eliminated from systemic circulation renally through a combination of glomerular filtration and active tubular secretion. Tenofovir is not a substrate for human organic cation transporter type 1 (hOCT1) or hOCT2. Tenofovir accumulates to fivefold lower levels in MRP4-overexpressing cells, and its accumulation could be increased by an MRP inhibitor. Tenofovir produces no significant changes in mitochondrial DNA (mtDNA) levels in human hepatoblastoma (HepG2) cells, skeletal muscle cells (SkMCs), or renal proximal tubule epithelial cells. Tenofovir elevates lactate production by less than 20% in HepG2 cells or SkMCs. Tenofovir is efficiently phosphorylated to tenofovir diphosphate (TFV-DP) in both HepG2 cells and primary human hepatocytes. Tenofovir has a 50% effective concentration of 1.1 mM against HBV in cell-based assays, and potency is improved > 50-fold by the addition of bis-isoproxil progroups. Tenofovir has previously demonstrated full activity against lamivudine-resistant HBV in vitro and clinically. Tenofovir inhibits the proliferation of liver-derived HepG2 cells and normal skeletal muscle cells with CC(50) values of 398 μM and 870 μM, respectively. Tenofovir shows substantially weaker effects on proliferation and viability of renal proximal tubule epithelial cells than cidofovir, a related nucleotide analog with the potential to induce renal tubular dysfunction.

In vivo


Cell Data

cell lines:

Concentrations:450 μM or 1,350 μM

Incubation Time:15 min to 12 h

Powder Purity:≥99%

规格

英文别名
Tenofovir DF | 2,4,6,8-Tetraoxa-5-phosphanonanedioic acid, 5-[[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]-, 1,9-bis(1-methylethyl) ester, 5-oxide, (2E)-2-butenedioate (1:1)
规格或纯度
10mM in DMSO
英文名称
Tenofovir (GS 1278) Disoproxil Fumarate
生化机理
富马酸替诺福韦二吡呋酯(GS-1278,Tenofovir DF)属于抗逆转录病毒药物,它通过与天然底物脱氧腺苷 5'-triphosphate 竞争,抑制 HIV 逆转录酶的活性,并在掺入 DNA 后终止 DNA 链。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
人体免疫缺陷病毒 1 型逆转录酶抑制剂
名称和识别符
EC号
687-766-5
分子类型
小分子
Isomeric SMILES
C[C@H](CN1C=NC2=C(N=CN=C21)N)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C.C(=C/C(=O)O)\C(=O)O
PubChem CID
分子量
635.51

技术文档

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高级数据

化学和物理性质
熔点
113-115°C
安全和危险性(GHS)
信号词
危险
危险声明

H318: 造成严重的眼睛损伤

H412: 对水生生物有害并具有长期持续影响

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