| Description | Tenofovir (GS 1278) is an adenine analog REVERSE TRANSC-RIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B. It is used to treat HIV INFECTIONS and CHRONIC HEPATITIS B, in combination with other ANTIVIRAL AGENTS, due to the emergence of ANTIVIRAL DRUG RESISTANCE when it is used alone. |
| In vitro | 皮下注射给药猪尾猕猴30 mg/kg Tenofovir通过猪尾猕猴的阴道内暴露完全消除HIV感染.30 mg/kg Tenofovir可以完全预防所有猕猴的SIV感染而无毒性.Tenofovir处理可以降低血浆病毒RNA水平到检测不到水平,同时降低外周血单核细胞和脑脊液（CSF）中血浆和感染细胞的感染性以及稳定CD4 + T细胞数量. |
| In vivo | 4 μM Tenofovir完全抑制MT-2细胞中HIVIIIB的生长。Tenofovir抑制HepG2 2.2.15,HepAD38和HepAD79细胞中乙型肝炎病毒（HBV）的活性。在MT-4细胞中减少HIV-1（IIIB）,HIV-2（ROD）和HIV（EHO）的病毒致细胞病变效应,EC50为1.15 μg/ mL,1.12 μg/ mL和1.05 μg/ mL。Tenofovir也降低SIV(mac251) ,SIV(B670) ,SHIV(89.6)和 SHIV(RTSHIV)的致细胞病变效应。Tenofovir对表达Q151M突变的多核苷耐药性HIV具有独特的活性,而对T69S插入突变的病毒敏感性降低。 |
| Cell experiments | Cells are plated into 48-well tissue culture plates (39,000 cells/mL) and allowed to grow for 48 h followed by treatment with vehicle or Tenofovir. Following the treatment period, cell viability is assessed using the MTT assay. The MTT assay relies on the conversion of tetrazolium dye 3-(4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to formazan by NAD(P)H-dependent oxidoreductases[1]. |
| Synonyms | 替诺福韦, 泰诺福韦, PMPA, TDF, GS 1278 |
| molecular weight | 287.21 |
| Molecular formula | C9H14N5O4P |
| CAS | 147127-20-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 4 mg/mL (13.92 mM), Heating is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: 2 mg/mL (6.96 mM) |
| References | 1. Witvrouw M, et al. Antivir Ther, 2004, 9(1), 57-65. 2. Miller MD, et al. Nucleosides Nucleotides Nucleic Acids, 2001, 20(4-7), 1025-1028. 3. Ying C, et al. J Viral Hepat, 2000, 7(2), 161-165. 4. Wainberg MA, et al. Antivir Ther, 1999, 4(2), 87-94. 5. De Clercq E, et al. Clin Microbiol Rev, 2003, 16(4), 569-596. 6. 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. 7. Wu Y, Yang J, Duan C, et al. Simultaneous determination of antiretroviral drugs in human hair with liquid chromatography-electrospray ionization-tandem mass spectrometry[J]. Journal of Chromatography B. 2018 Apr 15;1083:209-221. 8. Tan S, Li W, Li Z, et al. A Novel CXCR4 Targeting Protein SDF-1/54 as an HIV-1 Entry Inhibitor. Viruses. 2019, 11(9): 874. |
| Citations | 1. Tan S, Li W, Li Z, et al. A Novel CXCR4 Targeting Protein SDF-1/54 as an HIV-1 Entry Inhibitor. Viruses. 2019, 11(9): 874 2. Wu Y, Yang J, Duan C, et al. Simultaneous determination of antiretroviral drugs in human hair with liquid chromatography-electrospray ionization-tandem mass spectrometry. Journal of Chromatography B. 2018 Apr 15;1083:209-221 3. Bao H, Yan J, Huang J, et al.Activation of endogenous retrovirus triggers microglial immuno-inflammation and contributes to negative emotional behaviors in mice with chronic stress.Journal of Neuroinflammation.2023, 20(1): 1-16. 4. Wu M, Li M, Liu W, et al.Nucleoporin Seh1 maintains Schwann cell homeostasis by regulating genome stability and necroptosis.Cell Reports.2023, 42(7): 112802. |