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Tenofovir

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Chemical Structure| 147127-20-6 同义名 : 泰诺福韦 ;GS 1278;PMPA;TDF;(R)-PMPA;GS-1275
CAS号 : 147127-20-6
货号 : A193687
分子式 : C9H14N5O4P
纯度 : 95%
分子量 : 287.21
MDL号 : MFCD00943794
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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

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].
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
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 <<
实验方案
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
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.