Tenofovir Disoproxil|201341-05-1|(替诺福韦酯; Bis(POC)-PMPA; GS 4331)-陌孚医药/Medlife

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Tenofovir Disoproxil (Synonyms: 替诺福韦酯; Bis(POC)-PMPA; GS 4331)

目录号: PL03712 纯度: ≥99%

CAS No. :201341-05-1

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中文名称	Tenofovir Disoproxil
中文别名	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;富马酸泰诺福韦酯;富马酸替诺福韦酯杂质对照品;替诺福韦;替诺福韦酯杂质
英文名称	Tenofovir Disoproxil
英文别名	9-((R)-2-((Bis(((isopropoxycarbonyl)oxy)methoxy)phosphinyl)methoxy)propyl)adenine;Tenofovir;(R)-(((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)-bis(oxy))bis(methylene) diisopropyl dicarbonate;Bis(POC)-PMPA;GS 4331;GS-4331;Pmpa prodrug;Tdf;Bis(POC)PMPA;Tenofovir (Disoproxil);Tenofovir Disoproxil Fumarate;F4YU4LON7I;tenofovir bis(isopropyloxycarbonyloxymethyl) ester;Tenofovirdisoproxil;bis({[(propan-2-yloxy)carbonyl]oxy}methyl) ({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)phosphonate;C19H30N5O10P;9-[(r)-2-[[bis[[(isopropoxycarbonyl)oxy]methoxy]phosphinyl]methoxy]propy;Tenofovir Disoproxil
Cas No.	201341-05-1
分子式	C₁₉H₃₀N₅O₁₀P
分子量	519.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Tenofovir Disoproxil (Bis(POC)-PMPA) 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。

生物活性

Tenofovir Disoproxil (Bis(POC)-PMPA) is a nucleotide reverse transcriptase inhibitor 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.

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

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Murphy RA, et al. Establishment of HK-2 Cells as a Relevant Model to Study Tenofovir-Induced Cytotoxicity. Int J Mol Sci. 2017 Mar 1;18(3)
[2]. Musumeci G, et al. M48U1 and Tenofovir combination synergistically inhibits HIV infection in activated PBMCs and human cervicovaginal histocultures. Sci Rep. 2017 Feb 1;7:41018

溶解度数据	In Vitro: DMSO : ≥ 38 mg/mL (73.16 mM)配制储备液

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Data Sheet

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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