Tenofovir

製品コードS1401 バッチS140103

印刷

化学情報

Chemical Structure Synonyms GS-1278 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C9H14N5O4P
分子量 287.21 CAS No. 147127-20-6
Solubility (25°C)* 体外 Water 33 mg/mL (114.89 mM)
DMSO Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
30%propylene glycol 5%Tween80 65%D5W
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Tenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections.
in vitro Tenofovir reduces the viral cytopathic effect of HIV-1(IIIB), HIV-2(ROD) and HIV(EHO) with EC50 of 1.15 μg/mL, 1.12 μg/mL and 1.05 μg/mL in MT-4 cells. Tenofovir also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). [1] Tenofovir is uniquely active against multinucleoside-resistant HIV expressing the Q151M mutation, but shows reduced susceptibility to the T69S insertion mutations. [2] Tenofovir inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells. [3] Tenofovir (4 μM) completely inhibits the growth of HIVIIIB in MT-2 cells. Tenofovir inhibits synthesis of negative strand strong-stop DNA with IC50 of 9 µM for wild-type RT, 6 µM for M184V RT and 50 µM for K65R RT. [4]
in vivo Tenofovir (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. Tenofovir treatment reduces plasma viral RNA levels to undetectable, with parallel decreases in the infectivity of plasma and infectious cells in peripheral blood mononuclear cells and cerebrospinal fluid (CSF) and stabilization of CD4+ T-cell numbers. Tenofovir (30 mg/kg, s.c.) completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques. [5]
特徴 Tenofovir disoproxil fumarate is the prodrug form of tenofovir.

プロトコル(参考用のみ)

キナーゼアッセイ HIV inhibition
HIV-1 strains are evaluated by the MT-4/MTT assay for their susceptibility to the inhibitory effect of nucleoside reverse transcriptase inhibitors Tenofovir. Both SHIV isolates are derived from SIV(mac239), containing either the HIV-1(HXB2) envelope and the associated auxiliary HIV-1 vpu and rev genes (SHIV89.6), or the HIV-1(HXB2) RT gene (RTSHIV). Commonly used wild-type HIV-1(IIIB) strain is also tested for comparison. All virus stocks are used at comparable infectious virus titres, that is, 150–300 CCID50(cell culture infectious dose). All data are derived from at least two separate tests. Antiviral data are reported as the concentration of Tenofovir required to inhibit 50% virus-induced cell killing [50% effective concentration (EC50)]. The fold increase in the EC50 values of Tenofovir against the different HIV-2, SIV and SHIV strains is calculated in comparison with the EC50 against HIV-1(IIIB).
動物実験 動物モデル Macaques
投薬量 30 mg/kg
投与方法 Subcutaneously

カスタマーフィードバック

, , Sci Transl Med, 2014, 6(262):262ra157.

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Nucleos(t)ide analogs for hepatitis B virus infection differentially regulate the growth factor signaling in hepatocytes [ Hepatol Commun, 2024, 8(1)e0351] PubMed: 38180972
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Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] PubMed: 37310224
Reverse Transcriptase Inhibition Disrupts Repeat Element Life Cycle in Colorectal Cancer [ Cancer Discov, 2022, candisc.1117.2021] PubMed: 35320348
Characterization of the tenofovir resistance-associated mutations in the hepatitis B virus isolates across genotypes A to D [ Antiviral Res, 2022, 203:105348] PubMed: 35644506
In Vitro Susceptibility of HIV Isolates with High Growth Capability to Antiretroviral Drugs [ Int J Mol Sci, 2022, 23(23)15380] PubMed: 36499705
A cell-based assay to discover inhibitors of SARS-CoV-2 RNA dependent RNA polymerase [ Antiviral Res, 2021, S0166-3542(21)00068-1] PubMed: 33894278
Identification and characterization of a novel hepatitis B virus pregenomic RNA encapsidation inhibitor. [ Antiviral Res, 2020, 175:104709] PubMed: 31940474
Impact of vaginal microbiome communities on HIV antiretroviral-based pre-exposure prophylaxis (PrEP) drug metabolism [ PLoS Pathog, 2020, 16(12):e1009024] PubMed: 33270801
Sofosbuvir Activates EGFR-Dependent Pathways in Hepatoma Cells with Implications for Liver-Related Pathological Processes. [ Cells, 2020, 17;9(4) pii: E1003] PubMed: 32316635

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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