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Tenofovir Disoproxil Fumarate.
抗逆转录制剂(HIV-1 RT 抑制剂),Tenofovir Disoproxil Fumarate是用于治疗 HIV 和慢性乙型肝炎的核苷酸逆转录酶抑制剂
目录号: PC12813 纯度: ≥98%
CAS No. :202138-50-9
商品编号 规格 价格 会员价 是否有货 数量
PC12813-25mg 25mg ¥490.00 请登录
PC12813-100mg 100mg ¥1470.00 请登录
PC12813-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥686.00 请登录
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中文名称
Tenofovir Disoproxil Fumarate.
中文别名
富马酸替诺福韦酯;(R)-9-(2-磷酸甲氧基丙基)腺嘌呤二(异丙氧羰基氧甲基)酯富马酸盐;富马酸泰诺福韦酯;富马酸泰诺福韦酯(TDF);富马酸替诺福韦;富马酸替诺福韦酯 标准品;富马酸替诺福韦酯,Tenofovir disoproxil fumarate;富马酸替诺福韦酯标准品及杂质;富马酸替诺福韦酯原药;富马酸替诺福韦酯杂质及标准品;富马酸替诺富韦酯;他克莫司;泰诺福韦脂;泰诺福韦酯;泰诺福韦酯富马酸盐;泰诺福韦酯富马酸盐 USP标准品;替诺福韦;富马酸泰诺福韦二吡呋酯;替诺福韦富马酸
英文名称
Tenofovir Disoproxil Fumarate
英文别名
Tenofovir disoproxil fumarate;9-((R)-2-((Bis((( isopropoxycarbonyl)oxy) methoxy ) phosphinyl) methoxy) propyl) adenine fumarate;(R)-(((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)bis(oxy))bis(methylene) diisopropyl dicarbonate fumarate;Tenofovir DF;Tenofovir disoproxil;Tenofovir;Tenofovir diisoproxil fuMarate;TENOFOVIR DISOPROXIC;Bis(POC)PMPA fumarate;Bis{[(Isopropoxycarbonyl)oxy]methyl} ({[(2R)-1-(6-amino-9H-purin-9-yl)-2-propanyl]oxy}methyl)phosphonate fumarate;富马酸替诺福韦酯;DSSTox_RID_79447;DSSTox_CID_29808;DSSTox_GSID_50426;Tox21_112532;Tox21_113627;Tox21_113627_1;[[(2R)-1-(6-Aminopurin-9-yl)propan-2-yl]oxymethyl-(propan-2-yloxycarbonyloxymethoxy)phosphoryl]oxyme
Cas No.
202138-50-9
分子式
C23H34N5O14P
分子量
635.51
包装储存

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Tenofovir Disoproxil fumarate is a nucleotide reverse transcriptase inhibitor used to treat HIV and chronic Hepatitis B.

性状

Solid

IC50 & Target[1][2]

HIV-1

 

体外研究(In Vitro)

Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL, and is not toxic to PBMCs.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Tenofovir Disoproxil fumarate (20, 50, 140, or 300?mg/kg) administered to BLT mice, shows dose dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil fumarate (50, 140, 300?mg/kg) significantly reduces HIV transmission in BLT mice. Tenofovir Disoproxil fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil fumarate administration is safe and effective in the woodchuck model of chronic HBV infection.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : ≥ 50 mg/mL (78.68 mM)

H2O : 16.67 mg/mL (26.23 mM; Need ultrasonic and warming)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5735 mL 7.8677 mL 15.7354 mL
5 mM 0.3147 mL 1.5735 mL 3.1471 mL
10 mM 0.1574 mL 0.7868 mL 1.5735 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: PBS

    Solubility: 20 mg/mL (31.47 mM); Clear solution; Need ultrasonic

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.93 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.93 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.93 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.93 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.93 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.93 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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