富马酸替诺福韦酯 T2409L

Product Introduction
Bioactivity


英文名: Tenofovir Disoproxil Fumarate

描述: Tenofovir Disoproxil Fumarate (GS-1278 Disoproxil Fumarate) 是一种核苷酸逆转录酶抑制剂，有潜力研究艾滋病和慢性乙型肝炎。

细胞实验: 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.

激酶实验: HAT and HDAC Activity Assays :After homogenization of cardiac tissues, nucleoproteins are extracted using a Nuclear Extract Kit according to the manufacturer's instructions. HAT and HDAC activities of the nuclear protein extracts are determined using a colorimetric assay included in the HAT and HDAC assay kits.

动物实验: Tenofovir Disoproxil Fumarate is prepared in a placebo control. Twenty adult chronic WHV carrier woodchucks are stratified equally by age, sex, body weight, and serum GGT activity into five treatment groups consisting of four animals each: (i) Tenofovir Disoproxil Fumarate at 15.0 mg/kg once per day, (ii) Tenofovir Disoproxil Fumarate at 5.0 mg/kg/day, (iii) Tenofovir Disoproxil Fumarate at 1.5 mg/kg/day, (iv) Tenofovir Disoproxil Fumarate at 0.5 mg/kg/day, and (v) a placebo control. The woodchucks are treated daily for 4 weeks and observed for an additional 12 weeks following cessation of drug treatment.

体外活性: Tenofovir shows cytotoxic effects on cell viability in HK-2 cells in MTT assay (IC50: 9.21/2.77 μM at 48/72 h). Tenofovir lowers ATP levels in HK-2 cells. Tenofovir (3.0-28.8 μM) promotes protein carbonylation and oxidative stress in HK-2 cells. In addition, Tenofovir promotes apoptosis induced via mitochondrial damage in HK-2 cells. M48U1 and Tenofovir formulated in 0.25% HEC each inhibits the replication of both X4-tropic HIV-1IIIb and R5-tropic HIV-1BaL in activated PBMCs and inhibits patient-derived HIV-1 isolates and several laboratory strains. Aforesaid mixture exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL and is not toxic to PBMCs.

体内活性: Tenofovir Disoproxil Fumarate (20/50/140/300?mg/kg) administered to BLT mice, shows dose-dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil Fumarate (50/140/300?mg/kg) obviously lowers HIV transmission in BLT mice. Tenofovir Disoproxil Fumarate (0.5/1.5/5.0 mg/kg/day, p.o.) promotes a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil Fumarate administration is safe and effective in the woodchuck model of chronic HBV infection.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 44 mg/mL (69.23 mM)
DMSO : 50 mg/mL (78.68 mM)


关键字: Hepatitis B virus | HIV | HBV | GS 4331 | Inhibitor | GS4331 | Tenofovir Disoproxil Fumarate | GS-4331 | inhibit | Tenofovir Disoproxil | Reverse Transcriptase | Bis(POC)-PMPA | Human immunodeficiency virus

相关产品: Catalpol | Helioxanthin derivative 5-4-2 | Punicalagin | Thiamine hydrochloride | Kadsulignan L | Clevudine | HBV-IN-38 | Vesatolimod | Tenofovir Disoproxil | Linerixibat

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Orally Active Compound Library | NO PAINS Compound Library

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