Tenofovir maleate

Category	Human immunodeficiency Virus (HIV)
CAS	1236287-04-9
Description	Tenofovir hydrate 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 hydrate also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). Tenofovir hydrate inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells. Tenofovir hydrate (4 μM) completely inhibits the growth of HIVIIIB in MT-2 cells. Tenofovir hydrate inhibits synthesis of negative strand strong-stop DNA with IC50 of 9 ?M for wild-type RT, 6 ?M for M184V RT and 50 ?M for K65R RT. Tenofovir hydrate (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. Tenofovir hydrate 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 hydrate (30 mg/kg, s.c.) completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques.

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Product Information

Synonyms	Viread maleate; GS 1278 maleate; GS1278 maleate; GS-1278 maleate; PMPA maleate; TDF maleate
IUPAC Name	[(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethylphosphonic acid;(Z)-but-2-enedioic acid
Molecular Weight	403.28
Molecular Formula	C13H18N5O8P
Canonical SMILES	CC(CN1C=NC2=C1N=CN=C2N)OCP(=O)(O)O.C(=CC(=O)O)C(=O)O
InChI	InChI=1S/C9H14N5O4P.C4H4O4/c1-6(18-5-19(15,16)17)2-14-4-13-7-8(10)11-3-12-9(7)14;5-3(6)1-2-4(7)8/h3-4,6H,2,5H2,1H3,(H2,10,11,12)(H2,15,16,17);1-2H,(H,5,6)(H,7,8)/b;2-1-/t6-;/m1./s1
InChIKey	OPQKUDVCYGLXAH-REVJHSINSA-N
Purity	>98%
Solubility	In Vitro: 10 mM in DMSO
Appearance	Solid powder
Storage	Store at -20°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
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. 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.
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. 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.
Target	HIV; Reverse Transcriptase