Tenofovir Disoproxil Fumarate

Category	Hepatitis B Virus (HBV)
CAS	202138-50-9
Description	Tenofovir Disoproxil Fumarate belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5'-triphosphate.

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Product Information

Synonyms	GS-1278 Disoproxil Fumarate; GS 1278 Disoproxil Fumarate; GS1278 Disoproxil Fumarate
IUPAC Name	[[(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethyl-(propan-2-yloxycarbonyloxymethoxy)phosphoryl]oxymethyl propan-2-yl carbonate;(E)-but-2-enedioic acid
Molecular Weight	635.51
Molecular Formula	C19H30N5O10P.C4H4O4
Canonical SMILES	CC(C)OC(=O)OCOP(=O)(COC(C)CN1C=NC2=C(N=CN=C21)N)OCOC(=O)OC(C)C.C(=CC(=O)O)C(=O)O
InChI	InChI=1S/C19H30N5O10P.C4H4O4/c1-12(2)33-18(25)28-9-31-35(27,32-10-29-19(26)34-13(3)4)11-30-14(5)6-24-8-23-15-16(20)21-7-22-17(15)24;5-3(6)1-2-4(7)8/h7-8,12-14H,6,9-11H2,1-5H3,(H2,20,21,22);1-2H,(H,5,6)(H,7,8)/t14-;/m1./s1
InChIKey	VCMJCVGFSROFHV-PFEQFJNWSA-N
Boiling Point	642.7°C at 760 mmHg
Melting Point	113-115 °C (dec.)
Flash Point	342.5°C
Purity	98%
Density	1.45 g/cm3
Solubility	In Vitro: DMSO : ≥ 50 mg/mL (78.68 mM) H2O : 16.67 mg/mL (26.23 mM; Need ultrasonic and warming) In Vivo: 1.Add each solvent one by one: 10% DMSO >> 90% corn oil Solubility: ≥ 2.5 mg/mL (3.93 mM); Clear solution 2.Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline Solubility: ≥ 2.5 mg/mL (3.93 mM); Clear solution 3.Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (3.93 mM); Clear solution
Appearance	White to off-white solid
Storage	2 - 8°C
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.
Complexity	817
Exact Mass	635.18398777
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 and 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. 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.
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. It significantly reduces HIV transmission, and induces a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV.
PSA	269.85000
Target	HIV; Reverse Transcriptase; HBV
Vapor Pressure	2.06E-16mmHg at 25°C