Tenofovir Disoproxil Fumarate

别名: GS 1278, Tenofovir DF 中文名称：富马酸替诺福韦酯

目录号：S1400 Purity: 99.94%

Tenofovir Disoproxil Fumarate属于一类抗逆转录病毒药物，其通过与天然底物脱氧腺苷5’-三磷酸盐竞争以及整合到DNA后终止DNA链抑制HIV reverse transcriptase活性。

Tenofovir Disoproxil Fumarate Chemical Structure

CAS: 202138-50-9

规格	价格	库存
10mM (1mL in DMSO)	1056.27	现货
10mg	809.18	现货
50mg	2554.21	现货
1g	10401.3	现货
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产品质控

批次：纯度： 99.94%

99.94

Tenofovir Disoproxil Fumarate相关产品

相关靶点	HBV RT HIV RT RT	点击展开
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细胞实验数据示例

细胞系	实验类型	孵育时间	活性描述	文献信息
HepG2	Antiviral assay	9 days	Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay, IC50=5.1μM	17888662
HepG2	Cytotoxicity assay	9 days	Cytotoxicity against human HepG2 cells after 9 days by MTT assay, IC50=2.31μM	17888662
MT2	Function assay	5 days	Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days, EC50=0.015μM	17562366
human bone marrow cells	Cytotoxicity assay	24 hrs	Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay, CC50=0.9μM	20439609
human bone marrow cells	Cytotoxicity assay	24 hrs	Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay, CC50=1.9μM	20439609
HeLa-T4	Antiviral assay	48 hrs	Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC50=0.0029μM	21060108
HeLa-T4	Antiviral assay	48 hrs	Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC95=0.037μM	21060108
HeLaT4	Antiviral assay	24 hrs	Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated for 24 hrs followed by exposed to vi, EC50=0.12μM	21060108
HeLaT4	Function assay	24 hrs	Drug uptake in human HeLaT4 cells assessed as compound persist measured after 3 times washout at 100 time EC95 for HIV1 for 24 hrs	21060108
HeLaT4	Antiviral assay	24 hrs	Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated at 100 time EC95 for 24 hrs followed	21060108
PBMC	Antiviral assay	7 days	Antiviral activity against HIV1 infected in human PBMC assessed as inhibition of viral replication by measuring reverse transcriptase activity in cell supernatant preincubated with cells followed by viral infection measured after 7 days by radioactive inc, EC50=0.0046μM	27405794
HepG2.2.15	Antiviral assay	3 days	Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of viral DNA in cell supernatant incubated for 3 days in presence of 10% FBS followed by compound treatment in absence of 10% FBS for 3 days by qRT-PCR method, EC50=0.34μM	27405794
HepG2.2.15	Cytotoxicity assay	6 days	Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability after 6 days by XTT assay, CC50=29.2μM	27405794
PBMC	Antiviral assay	30 mins	Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human PHA-stimulated PBMC assessed as inhibition of viral replication by measuring reduction in p24 antigen production preincubated with cells for 30 mins followed by viral infection measured, IC50=0.08μM	28682067
PBMC	Antiviral assay	30 mins	Antiviral activity against CCR5 tropic HIV1 BaL infected in human PHA-stimulated PBMC assessed as inhibition of viral replication by measuring reduction in p24 antigen production preincubated with cells for 30 mins followed by viral infection measured on , IC50=0.22μM	28682067
MT4	Antiviral assay	6 days	Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 6 days by XTT dye based assay, EC50=4.89μM	28682067
MT4	Antiviral assay	6 days	Antiviral activity against tenofovir-resistant CXCR4-tropic HIV-1 NL4-3 harboring reverse transcriptase K65R mutant infected in human MT4 cells assessed as inhibition of viral replication inhibition of virus-induced cytopathic effect after 6 days by XTT d, EC50=11.3μM	28682067
MT2	Antiviral assay		Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication, IC50=0.54μM	19596885
MT-2	Antiviral assay		Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, EC50=0.0068μM	19104010
HeLa P4/R5	Antiviral assay		Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=4.7μM	19596885
HeLa P4/R5	Antiviral assay		Antiviral activity against HIV1 harboring reverse transcriptase K65R mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=11.4μM	19596885
HeLaT4	Antiviral assay		Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of 2 mins magnetic nanopartials-medated infection in human HeLaT4 cells treated for 1, EC99.6=0.95μM	21060108
HeLaT4	Cytotoxicity assay		Cytotoxicity against human HeLaT4 cells by WST-1 assay, CC50=34μM	21060108
HepG2.2.15	Antiviral assay		Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic DNA synthesis by reed and munch method, IC50=0.85μM	31223460
HepG2.2.15	Cytotoxicity assay		Cytotoxicity against human HepG2.2.15 cells infected with HBV, CC50=20.71μM	31223460
点击查看更多细胞系数据

生物活性

产品描述

靶点

HIV reverse transcriptase ^[1]
(Cell-free assay)

体外研究(In Vitro)
体外研究活性	Tenofovir的循环经肾脏通过肾小球滤过和肾小管主动分泌。Tenofovir不是人有机阳离子转运1型（hOCT1）或hOCT2的底物。在MRP4过表达细胞中，Tenofovir积累到五倍较低水平，MRP抑制剂可提高其累积。^[1] 在人肝母细胞瘤（肝癌）细胞，骨骼肌细胞（SkMCs）或肾近端小管上皮细胞中，Tenofovir并不显著影响线粒体DNA（mtDNA）的。在HepG2细胞或SkMCs中，Tenofovir升高的乳酸生产小于20％。^[2] 在HepG2细胞和人原代肝细胞中，Tenofovir是替诺福韦二磷酸（TFV-DP）有效的磷酸化。在基于细胞的测定中，Tenofovir抗HBV的50％有效浓度是1.1 mM，加入bis-isoproxil前基团之后有效率提高50倍。在体外和临床中，Tenofovir对lamivudine耐药HBV有充分的活动。^[3] Tenofovir抑制肝源性肝癌细胞和正常骨骼肌细胞的增殖，CC（50）值分别为398 μM和870 μM。Tenofovir比cidofovir对肾近曲小管上皮细胞的增殖和生存能力影响弱，cidofovir具有潜在的相关的核苷酸类似物诱导肾小管功能障碍。^[4]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05874440	Recruiting	Chronic Hepatitis b Patients	Sohag University	April 15 2023	--
NCT03576066	Completed	Chronic Hepatitis B	Assembly Biosciences	June 11 2018	Phase 2
NCT03361956	Completed	Hepatitis B	Janssen Sciences Ireland UC	February 13 2018	Phase 2
NCT02985996	Completed	HIV Infections	Emory University\|Centers for Disease Control and Prevention	February 6 2017	Phase 1

参考文献
[1] Ray AS, et al. Antimicrob Agents Chemother, 2006, 50(10), 3297-3304. [2] Birkus G, et al. Antimicrob Agents Chemother, 2002, 46(3), 716-723. [3] Delaney WE 4th, et al. Antimicrob Agents Chemother, 2006, 50(7), 2471-2477. [4] Cihlar T, et al. Antiviral Res, 2002, 54(1), 37-45. [5] Taneva E, et al. Antimicrob Agents Chemother. 2015, 60(3):1667-75. [6] Ng HH, et al. Int J Toxicol. 2015, 34(1):4-10. + 展开

参考文献

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化学信息&溶解度

分子量	635.51	分子式	C₁₉H₃₀N₅O₁₀P.C₄H₄O₄
CAS号	202138-50-9	SDF	Download Tenofovir Disoproxil Fumarate SDF
Smiles	CC(C)OC(=O)OCOP(=O)(COC(C)CN1C=NC2=C(N=CN=C21)N)OCOC(=O)OC(C)C.C(=CC(=O)O)C(=O)O
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 100 mg/mL ( (157.35 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 100 mg/mL (157.35 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (157.35 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 4 mg/mL (6.29 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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