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Tenofovir Disoproxil

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Chemical Structure| 201341-05-1 同义名 : Bis(POC)-PMPA;GS 4331
CAS号 : 201341-05-1
货号 : A119233
分子式 : C19H30N5O10P
纯度 : 98%
分子量 : 519.443
MDL号 : MFCD00952920
存储条件:

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 40 mg/mL(77.01 mM),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

动物实验配方:
生物活性
描述 Tenofovir exhibits cytotoxicity in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 hours in the MTT assay, respectively. It reduces ATP levels and increases oxidative stress and protein carbonylation within the concentration range of 3.0 to 28.8 μM in HK-2 cells. Additionally, Tenofovir triggers apoptosis via mitochondrial damage in HK-2 cells [1]. Tenofovir and M48U1, each formulated in 0.25% HEC, collectively inhibit the replication of R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, as well as various laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC demonstrates synergistic antiretroviral activity against R5-tropic HIV-1BaL infection without PBMC toxicity [2].
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
NCT02287857 Chronic Hepatitis B Not Applicable Recruiting October 2019 China, Beijing ... 展开 >> Beijing Ditan Hospital Capital Medical University Recruiting Beijing, Beijing, China, 100015 Contact: Xiao hua Hao, doctor    13466590802    xiaohualuck@sina.com    Peking University First Hospital Recruiting Beijing, Beijing, China, 100034 Contact: Li qin Yu, doctor    010-66119025    jgbgs090101@126.com    Peking University People's Hospital Recruiting Beijing, Beijing, China, 100044 Contact: Hao Wang, doctor    010-88325988    jgbgs090101@126.com    Beijing You An Hospital, Capital Medical University Recruiting Beijing, Beijing, China, 100069 Contact: Mei xia Wang, doctor    010-83997322    youangcp@163.com    China, Chongqing First Affiliated Hospital, Third Military Medical University Recruiting Chongqing, Chongqing, China, 400039 Contact: Yong chuan Chen, doctor    13883405537    zwmcyc@163.com    China, Guangdong Third Affiliated Hospital of Sun Yat-sen Recruiting Guangzhou, Guangdong, China, 510630 Contact: Qian Huang, doctor    02085253153    sankyk@163.com    China, Henan Henan Provincial People's Hospital Recruiting Zhengzhou, Henan, China, 450003 Contact: Xiu Jin, doctor    13526660319       First Affiliated Hospital of Zhengzhou University Recruiting Zhengzhou, Henan, China, 450052 Contact: Juan Li, doctor    13526506270       China, Jiangsu The Second Hospital of Nanjing Recruiting Nanjing, Jiangsu, China, 210003 Contact: Yu Pan, doctor    13814099474       First Affiliated Hospital of Nanjing Medical University Recruiting Nanjing, Jiangsu, China Contact: Xu Huang, doctor    02568136360    jsphkj@163.com    China, Shanghai Ruijin Hospital Shanghai Jiaotong University School of Medicine Recruiting Shanghai, Shanghai, China, 200025 Contact: Yi feng Wang, doctor    02154661789    ruijin_gcp@126.com    Huashan Hospital, Fudan University Recruiting Shanghai, Shanghai, China, 200040 Contact: Fei Dong, doctor    02152888041       Shanghai Public Health Clinical Center Recruiting Shanghai, Shanghai, China, 201508 Contact: Na Li, doctor    18916082023    lina40125@shaphc.org    China, Sichuan West China Hospital of Sichuan University Recruiting Chengdou, Sichuan, China, 610041 Contact: Juan Liao, doctor    15828323384    hxcrgcp@163.com    China, Zhejiang First Affiliated Hospital of Zhejiang University School of Medicine Recruiting Hangzhou, Zhejiang, China Contact: Li hua Wu, doctor    13819195192 收起 <<
NCT03251144 HIV/AIDS Anti... 展开 >>viral Toxicity Antiviral Drug Adverse Reaction Mitochondrial Alteration 收起 << Phase 1 Phase 2 Recruiting July 31, 2020 United States, California ... 展开 >> UCLA CARE Center Recruiting Los Angeles, California, United States, 90035 Contact: Theodoros Kelesidis, MD, PhD, Msc    310-825-7225    tkelesidis@mednet.ucla.edu 收起 <<
NCT03236610 Proportion of Patients With a ... 展开 >>Sustained Virological Response (Serum HBV DNA <20 IU/mL) at Week 48 收起 << Phase 3 Recruiting June 30, 2019 Korea, Republic of ... 展开 >> Uijeongbu St. Mary Hospital Recruiting Uijongbu, Korea, Republic of Contact: Chang Wook Kim    82318203997    cwkim@catholic.ac.kr 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.63mL

1.93mL

0.96mL

19.25mL

3.85mL

1.93mL

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.