Tenofovir Disoproxil Fumarate Bioactivity,Chemical Properties,Storage & Solubility Information Pathways-PeptideDB

Description	Tenofovir Disoproxil Fumarate (GS-1278 Disoproxil Fumarate) is a pro-drug, fumaric acid salt form of tenofovir, a nucleoside reverse transcriptase inhibitor analog of adenosine. Tenofovir disoproxil fumarate is prescribed to treat HIV and chronic hepatitis B virus (HBV) in adults.
In vitro	Tenofovir在MTT实验中对HK-2细胞的存活能力表现出细胞毒性效应（IC50: 9.21/2.77 μM在48/72小时）。该化合物降低HK-2细胞中的ATP水平，并在3.0-28.8 μM浓度范围内促进蛋白质羰基化和氧化应激。此外，Tenofovir还通过线粒体损伤促进HK-2细胞的凋亡。在0.25% HEC中配制的M48U1和Tenofovir能够抑制活化的PBMCs中X4-热性HIV-1IIIb与R5-热性HIV-1BaL的复制，并抑制患者源HIV-1分离物及多个实验室株。上述混合物对R5-热性HIV-1BaL感染表现出协同的抗逆转录病毒活性，对PBMCs无毒性。
In vivo	Tenofovir Disoproxil Fumarate（20/50/140/300mg/kg）在BLT人源化小鼠的阴道HIV挑战实验中表现出剂量依赖性活性。Tenofovir Disoproxil Fumarate（50/140/300mg/kg）显著降低了BLT小鼠中HIV的传播率。此外，Tenofovir Disoproxil Fumarate（0.5/1.5/5.0 mg/kg/day，p.o.）在慢性感染WHV的旱獭中促进了血清病毒量剂量依赖性下降。Tenofovir Disoproxil Fumarate的应用在慢性HBV感染的旱獭模型中被证明是安全且有效的。
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.
Animal experiments	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.
Synonyms	GS-1278 Disoproxil Fumarate, Tenofovir DF, 富马酸替诺福韦酯
molecular weight	635.51
Molecular formula	C19H30N5O10P·C4H4O4
CAS	202138-50-9
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
Solubility	H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 44 mg/mL (69.23 mM) DMSO: 50 mg/mL (78.68 mM)
References	1. Ray AS, et al. Antimicrob Agents Chemother, 2006, 50(10), 3297-3304. 2. Birkus G, et al. Antimicrob Agents Chemother, 2002, 46(3), 716-723. 3. Delaney WE 4th, et al. Antimicrob Agents Chemother, 2006, 50(7), 2471-2477. 4. Cihlar T, et al. Antiviral Res, 2002, 54(1), 37-45. 5. 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.
Citations	1. 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.

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Tenofovir Disoproxil Fumarate

CAS No.: 202138-50-9