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替诺福韦 /Tenofovir {[allProObj[0].p_purity_real_show]}

货号:A193687 同义名: 泰诺福韦 / GS 1278;PMPA

Tenofovir is an antiretroviral drug known as nucleotide analogue reverse transcriptase inhibitors (NRTIs), which block reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Tenofovir 化学结构 CAS号:147127-20-6
Tenofovir 化学结构
CAS号:147127-20-6
Tenofovir 3D分子结构
CAS号:147127-20-6
Tenofovir 化学结构 CAS号:147127-20-6
Tenofovir 3D分子结构 CAS号:147127-20-6
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Tenofovir 纯度/质量文件 产品仅供科研

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Tenofovir 生物活性

描述 Tenofovir (GS 1278) is employed as a nucleotide reverse transcriptase inhibitor for treating HIV and chronic Hepatitis B (HBV) [1].
体内研究

Tenofovir Disoproxil Fumarate administered at varying doses (20, 50, 140, or 300 mg/kg) shows dose-dependent efficacy in preventing vaginal HIV transmission in BLT humanized mice. At 50, 140, and 300 mg/kg, it significantly reduces HIV transmission [3].

Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, pO.) results in a dose-dependent reduction of serum viremia in woodchucks with chronic WHV infection, proving safe and effective in this model of chronic HBV infection [4].

体外研究

Tenofovir reduces HK-2 cells viability with IC50 values of 9.21 μM at 48 hours and 2.77 μM at 72 hours in MTT assays. It decreases ATP levels, elevates oxidative stress and protein carbonylation, and induces apoptosis through mitochondrial damage in these cells [1].

Tenofovir combined with M48U1, each formulated in 0.25% HEC, inhibits replication of R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs. This formulation also inhibits various laboratory and patient-derived HIV-1 strains, displaying synergistic antiretroviral activity against R5-tropic HIV-1BaL infection without toxicity to PBMCs [2].

Tenofovir 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
C3H/3T3 cells Function assay 6 days Inhibition of murine sarcoma virus-induced transformation of mouse embryo fibroblast C3H/3T3 cells after 6 days, EC50=0.23 μM 18556209
C8166 cells Function assay 4 days Antiviral activity against 100 TCID50 wild-type Human immunodeficiency virus type 2 ROD infected in C8166 cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis, EC50=7.1 μM 21803462
CEM (human leukemia) cells Function assay Antiviral activity against HIV-1 (IIIB) in CEM (human leukemia) cells, EC50=1.2 μM 14584956
CHO cells Cytotoxicity assay 120 h Cytotoxicity against CHO cells after 120 hrs by Cell-Titer Glo assay, CC50=21 μM 19001108

Tenofovir 动物研究

Dose Mice: 20 mg/kg - 300 mg/kg[3] (i.p.), 50 mg/kg - 1000 mg/kg[4] (p.o.) Woodchucks: 0.5 mg/kg - 5 mg/kg (p.o.)
Administration i.p., p.o.

Tenofovir 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01488526 Hepatitis B Infection ... 展开 >> Chronic Infection Viremia 收起 << Phase 4 Active, not recruiting October 28, 2017 China, Chongqing ... 展开 >> Southwest Hospital Chongqing, Chongqing, China, 400038 China, Hebei The Fifth Hospital of Shijiazhuang Shijiazhuang, Hebei, China, 050021 China, Henan Nanyang Central Hospital Nanyang, Henan, China, 473000 China, Jiangsu The Second Affiliated Hospital of the Southeast University Nanjing, Jiangsu, China, 210003 China, Jilin Hepatobiliary Disease Hospital of Jilin Province Chang Chun, Jilin, China, 130062 收起 <<
NCT03270969 HIV Prevention Phase 1 Active, not recruiting December 2018 United States, Nebraska ... 展开 >> Specialty Care Center Omaha, Nebraska, United States, 68106 收起 <<
NCT00528957 HIV Infections Phase 3 Completed - United States, California ... 展开 >> Jeffrey Goodman Special Care Clinic Los Angeles, California, United States, 90027 University California Los Angeles, School of Medicine, Pediatric, Infectious Diseases Los Angeles, California, United States, 90095 United States, Florida Children's Diagnostic and Treatment Center, Inc Fort Lauderdale, Florida, United States, 33316 University of Florida, Jacksonville Jacksonville, Florida, United States, 32209 United States, Pennsylvania St. Christopher's Hospital for Children Philadelphia, Pennsylvania, United States, 19134 United States, Tennessee St. Jude Children's Research Hospital Memphis, Tennessee, United States, 38105 Panama Hospital del Nino Panama City, Panama United Kingdom Great Ormond Street Hospital London, United Kingdom Imperial College London, Paediatrics Infectious Diseases London, United Kingdom 收起 <<

Tenofovir 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.

[3]Wahl A, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model. Sci Rep. 2017 Feb 1;7:41098.

[4]Menne S, Cote PJ, Korba BE, Antiviral effect of oral administration of tenofovir disoproxil fumarate in woodchucks with chronic woodchuck hepatitis virus infection. Antimicrob Agents Chemother. 2005 Jul;49(7):2720-8.

Tenofovir 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.48mL

0.70mL

0.35mL

17.41mL

3.48mL

1.74mL

34.82mL

6.96mL

3.48mL

Tenofovir 技术信息

CAS号147127-20-6
分子式C9H14N5O4P
分子量 287.21
别名 泰诺福韦 ;GS 1278;PMPA;TDF;(R)-PMPA;GS-1275
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 6 mg/mL(20.89 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 2 mg/mL(6.96 mM),配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 20 mg/mL suspension

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