Tenofovir Disoproxil Fumarate

Research use only, not for human use.

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

Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.(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.

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.

Tenofovir Disoproxil fumarate (20, 50, 140, or 300mg/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.

Bis(POC)-PMPA

Microbiology/Virology

HIV

HIV reverse transcriptase

Infection

——

202138-50-9

635.51

C19H30N5O10P·C4H4O4

>98% (HPLC)

DMSO:128 mg/mL (201.41 mM)

C(\C=C\C(=O)O)(=O)O.C(OCOP(=O)(CO[C@@H](CN1C2=NC=NC(=C2N=C1)N)C)OCOC(OC(C)C)=O)(OC(C)C)=O

——

(-20℃)

With Ice Pack

≥ 2 years