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Tenofovir hydrate

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Chemical Structure| 206184-49-8 同义名 : PMPA hydrate;GS 1278 hydrate
CAS号 : 206184-49-8
货号 : A137641
分子式 : C9H16N5O5P
纯度 : 98%+
分子量 : 305.23
MDL号 : MFCD11519982
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(16.38 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 demonstrates cytotoxic effects in HK-2 cells, with IC50 values of 9.21 μM at 48 hours and 2.77 μM at 72 hours in MTT assays. It lowers ATP levels, increases 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 both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, including several laboratory and patient-derived HIV-1 strains. This combination exhibits synergistic antiretroviral effects against R5-tropic HIV-1BaL infection and is non-toxic to PBMCs [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
NCT01475851 Hepatitis B, Chronic Phase 3 Completed - Japan ... 展开 >> GSK Investigational Site Aichi, Japan, 466-8560 GSK Investigational Site Aichi, Japan, 467-8602 GSK Investigational Site Chiba, Japan, 260-8677 GSK Investigational Site Fukuoka, Japan, 803-8505 GSK Investigational Site Hiroshima, Japan, 734-8551 GSK Investigational Site Hokkaido, Japan, 060-0033 GSK Investigational Site Kagoshima, Japan, 890-8520 GSK Investigational Site Kanagawa, Japan, 213-8587 GSK Investigational Site Miyagi, Japan, 980-8574 GSK Investigational Site Tokyo, Japan, 105-8470 GSK Investigational Site Tokyo, Japan, 180-8610 收起 <<
NCT01475851 - Completed - -
NCT01480284 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.28mL

0.66mL

0.33mL

16.38mL

3.28mL

1.64mL

32.76mL

6.55mL

3.28mL
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.