Tenofovir disoproxil

Modify Date: 2024-01-01 23:02:17

Tenofovir disoproxil structure	Common Name	Tenofovir disoproxil
	CAS Number	201341-05-1	Molecular Weight	519.443
	Density	1.5±0.1 g/cm3	Boiling Point	642.7±65.0 °C at 760 mmHg
	Molecular Formula	C₁₉H₃₀N₅O₁₀P	Melting Point	N/A
	MSDS	N/A	Flash Point	342.5±34.3 °C

Use of Tenofovir disoproxil

Tenofovir dsoproxil is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.

Name	tenofovir disoproxil
Synonym	More Synonyms

Description	Tenofovir dsoproxil is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
Related Catalog	Signaling Pathways >> Anti-infection >> HBV Signaling Pathways >> Anti-infection >> HIV Signaling Pathways >> Anti-infection >> Reverse Transcriptase Research Areas >> Cancer
In Vitro	Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage[1]. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL, and is not toxic to PBMCs[2].
In Vivo	Tenofovir Disoproxil Fumarate (20, 50, 140, or 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) significantly reduces HIV transmission in BLT mice[3]. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces 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[4].
Cell Assay	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 Admin	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.
References	[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.

Density	1.5±0.1 g/cm3
Boiling Point	642.7±65.0 °C at 760 mmHg
Molecular Formula	C₁₉H₃₀N₅O₁₀P
Molecular Weight	519.443
Flash Point	342.5±34.3 °C
Exact Mass	519.173035
PSA	195.25000
LogP	2.04
Vapour Pressure	0.0±1.9 mmHg at 25°C
Index of Refraction	1.578
Storage condition	-20°C

Hazard Codes	Xi

Tenofovir disoproxil

bis({[(propan-2-yloxy)carbonyl]oxy}methyl) ({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)phosphonate

Bis{[(isopropoxycarbonyl)oxy]methyl} ({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)phosphonate

Tdf

Bis{[(isopropoxycarbonyl)oxy]methyl} ({[(2R)-1-(6-amino-9H-purin-9-yl)-2-propanyl]oxy}methyl)phosphonate

Pmpa prodrug

Bis(((isopropoxycarbonyl)oxy)methyl) (((1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy)methyl)phosphonate

Carbonic acid, [[[[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl][[[(1-methylethoxy)carbonyl]oxy]methoxy]phosphinyl]oxy]methyl 1-methylethyl ester

Tenofovir (Disoproxil)