1. Anti-infection
  2. Reverse Transcriptase HIV HBV
  3. Tenofovir

Tenofovir  (Synonyms: GS 1278; PMPA)

Cat. No.: HY-13910 Purity: 99.89%
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Tenofovir (GS 1278) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV).

For research use only. We do not sell to patients.

Tenofovir Chemical Structure

Tenofovir Chemical Structure

CAS No. : 147127-20-6

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Tenofovir:

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Description

Tenofovir (GS 1278) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV)[1].

IC50 & Target

HIV-1

 

Cellular Effect
Cell Line Type Value Description References
Bone marrow cell CC50
3.5 μM
Compound: 2, TFV
Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay
Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay
[PMID: 20439609]
Bone marrow cell CC50
4.7 μM
Compound: 2, TFV
Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay
Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay
[PMID: 20439609]
C3H/3T3 EC50
0.23 μM
Compound: (R)-PMPA, Tenofovir
Inhibition of murine sarcoma virus-induced transformation of mouse embryo fibroblast C3H/3T3 cells after 6 days
Inhibition of murine sarcoma virus-induced transformation of mouse embryo fibroblast C3H/3T3 cells after 6 days
[PMID: 18556209]
C8166 EC50
7.1 μM
Compound: (R)-PMPA, Tenofovir
Antiviral activity against 100 TCID50 wild-type Human immunodeficiency virus type 2 ROD infected in C8166 cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
Antiviral activity against 100 TCID50 wild-type Human immunodeficiency virus type 2 ROD infected in C8166 cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
[PMID: 21803462]
CCRF-CEM CC50
> 100 μM
Compound: Tenofovir
Cytotoxicity against human CEM cells assessed as cell count after 3 days
Cytotoxicity against human CEM cells assessed as cell count after 3 days
[PMID: 26513643]
CCRF-CEM CC50
> 250 μM
Compound: (R)-PMPA
Cytotoxicity against human CEM cells assessed as inhibition of cell proliferation after 72 hrs by coulter counter analysis
Cytotoxicity against human CEM cells assessed as inhibition of cell proliferation after 72 hrs by coulter counter analysis
[PMID: 21429755]
CCRF-CEM EC50
3.2 μM
Compound: (R)-PMPA
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as inhibition of virus-induced syncytium formation after 4 to 5 days by microscopic analysis
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as inhibition of virus-induced syncytium formation after 4 to 5 days by microscopic analysis
[PMID: 21429755]
CCRF-CEM EC50
3.7 μM
Compound: Tenofovir
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
[PMID: 26513643]
CCRF-CEM EC50
3.7 μM
Compound: Tenofovir
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as reduction in virus-induced cytopathicity after 4 to 5 days by microscopy based syncytium cell formation assay
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as reduction in virus-induced cytopathicity after 4 to 5 days by microscopy based syncytium cell formation assay
[PMID: 25617695]
CCRF-CEM EC50
3.7 μM
Compound: 2, (R)-PMPA
Antiviral activity against Human immunodeficiency virus type 2 ROD infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
Antiviral activity against Human immunodeficiency virus type 2 ROD infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
[PMID: 24686012]
CCRF-CEM EC50
3.9 μM
Compound: Tenofovir
Antiviral activity against HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
Antiviral activity against HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
[PMID: 26513643]
CCRF-CEM EC50
3.9 μM
Compound: Tenofovir
Antiviral activity against HIV1 3B infected in human CEM cells assessed as reduction in virus-induced cytopathicity after 4 to 5 days by microscopy based syncytium cell formation assay
Antiviral activity against HIV1 3B infected in human CEM cells assessed as reduction in virus-induced cytopathicity after 4 to 5 days by microscopy based syncytium cell formation assay
[PMID: 25617695]
CCRF-CEM EC50
3.9 μM
Compound: 2, (R)-PMPA
Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
[PMID: 24686012]
CCRF-CEM EC50
4.1 μM
Compound: (R)-PMPA, Tenofovir
Antiviral activity against 100 TCID50 wild-type Human immunodeficiency virus 1 3B infected in CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
Antiviral activity against 100 TCID50 wild-type Human immunodeficiency virus 1 3B infected in CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
[PMID: 21803462]
CCRF-CEM EC50
4.6 μM
Compound: (R)-PMPA
Antiviral activity against HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced syncytium formation after 4 to 5 days by microscopic analysis
Antiviral activity against HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced syncytium formation after 4 to 5 days by microscopic analysis
[PMID: 21429755]
CCRF-CEM IC50
6.9 μM
Compound: 2, (R)-PMPA
Cytostatic activity against human CEM cells after 72 hrs by coulter counting analysis
Cytostatic activity against human CEM cells after 72 hrs by coulter counting analysis
[PMID: 24686012]
CHO CC50
173 μM
Compound: Tenofovir
Ratio of CC50 for CHO cells to CC50 for CHO cells expressing hOAT1 after 120 hrs by Cell-Titer Glo assay
Ratio of CC50 for CHO cells to CC50 for CHO cells expressing hOAT1 after 120 hrs by Cell-Titer Glo assay
[PMID: 19001108]
CHO CC50
21 μM
Compound: Tenofovir
Cytotoxicity against CHO cells after 120 hrs by Cell-Titer Glo assay
Cytotoxicity against CHO cells after 120 hrs by Cell-Titer Glo assay
[PMID: 19001108]
CHO CC50
435 μM
Compound: Tenofovir
Cytotoxicity against CHO cells expressing hOAT1 after 120 hrs by Cell-Titer Glo assay
Cytotoxicity against CHO cells expressing hOAT1 after 120 hrs by Cell-Titer Glo assay
[PMID: 19001108]
H9 CC50
> 100 μM
Compound: (R)-PMPA, Tenofovir
Cytotoxicity against PAP-activated human H9 cells on day 7 by MTT assay
Cytotoxicity against PAP-activated human H9 cells on day 7 by MTT assay
[PMID: 21803462]
H9 EC50
0.23 μM
Compound: (R)-PMPA, Tenofovir
Antiviral activity against 125 TCID50 wild type HIV1 LAI infected in human H9 cells assessed as reduction in viral replication measured on day 7 post infection by reverse transcriptase activity
Antiviral activity against 125 TCID50 wild type HIV1 LAI infected in human H9 cells assessed as reduction in viral replication measured on day 7 post infection by reverse transcriptase activity
[PMID: 21803462]
H9 EC50
8.3 μM
Compound: (R)-PMPA, Tenofovir
Antiviral activity against 6250 TCID50 wild type HIV1 LAI infected in human H9 cells assessed as reduction in viral replication measured on day 7 post infection by reverse transcriptase activity
Antiviral activity against 6250 TCID50 wild type HIV1 LAI infected in human H9 cells assessed as reduction in viral replication measured on day 7 post infection by reverse transcriptase activity
[PMID: 21803462]
HEK-293T CC50
> 100 μM
Compound: PMPA
Cytotoxicity against human 293T cells assessed as inhibition of cell proliferation by tetrazolium dye method
Cytotoxicity against human 293T cells assessed as inhibition of cell proliferation by tetrazolium dye method
[PMID: 17470654]
HEK-293T CC50
> 100 μM
Compound: TFV
Cytotoxicity against HEK293T cells assessed as reduction in cell viability in absence of HSA measured after 48 hrs by CellTiter 96 Aqueous One Solution reagent based cell proliferation assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability in absence of HSA measured after 48 hrs by CellTiter 96 Aqueous One Solution reagent based cell proliferation assay
[PMID: 34459598]
HEK-293T CC50
35.4 μM
Compound: TFV
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 48 hrs by CellTiter 96 Aqueous One Solution reagent based cell proliferation assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 48 hrs by CellTiter 96 Aqueous One Solution reagent based cell proliferation assay
[PMID: 34459598]
HeLa IC50
17 μM
Compound: 2, (R)-PMPA
Cytostatic activity against human HeLa cells after 72 hrs by coulter counting analysis
Cytostatic activity against human HeLa cells after 72 hrs by coulter counting analysis
[PMID: 24686012]
HepG2 CC50
> 100 μM
Compound: PMPA, tenofovir
Cytotoxicity against human HepG2 cells by MTS assay
Cytotoxicity against human HepG2 cells by MTS assay
[PMID: 17646420]
HepG2 IC50
12.3 μM
Compound: PMPA, 2
Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay
Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay
[PMID: 17888662]
HepG2 2.2.15 CC50
> 1716 μM
Compound: Tf
Cytotoxicity against human HepG2.2.15 cells by MTT assay
Cytotoxicity against human HepG2.2.15 cells by MTT assay
[PMID: 24731274]
HepG2 2.2.15 CC50
> 1740.95 μM
Compound: TF
Cytotoxicity against human HepG2(2.2.15) cells by modified-MTT assay
Cytotoxicity against human HepG2(2.2.15) cells by modified-MTT assay
[PMID: 22687441]
HepG2 2.2.15 IC50
> 1742.2 μM
Compound: Tenofovir
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as surface antigen HBsAg secretion after 72 hrs by ELISA
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as surface antigen HBsAg secretion after 72 hrs by ELISA
[PMID: 25737008]
HepG2 2.2.15 IC50
> 1742.2 μM
Compound: Tenofovir
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as surface antigen HBeAg secretion after 72 hrs by ELISA
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as surface antigen HBeAg secretion after 72 hrs by ELISA
[PMID: 25737008]
HepG2 2.2.15 CC50
> 1742.2 μM
Compound: Tenofovir
Cytotoxicity against human HepG 2.2.15 cells by MTT assay
Cytotoxicity against human HepG 2.2.15 cells by MTT assay
[PMID: 25737008]
HepG2 2.2.15 CC50
> 1820.42 μM
Compound: TF
Cytotoxicity against human HepG2(2.2.15) cells by MTT assay
Cytotoxicity against human HepG2(2.2.15) cells by MTT assay
[PMID: 22472044]
HepG2 2.2.15 CC50
> 300 μM
Compound: PMPA, tenofovir
Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red uptake assay
Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red uptake assay
[PMID: 17646420]
HepG2 2.2.15 IC50
0.68 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication by PCR analysis
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication by PCR analysis
[PMID: 22687441]
HepG2 2.2.15 IC50
0.77 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication by RT-PCR analysis
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication by RT-PCR analysis
[PMID: 22472044]
HepG2 2.2.15 CC50
1.85 mM
Compound: TF
Cytotoxicity against human HepG2(2.2.15) cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2(2.2.15) cells after 72 hrs by MTT assay
[PMID: 25737009]
HepG2 2.2.15 IC50
1160.23 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral e antigen secretion by ELISA
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral e antigen secretion by ELISA
[PMID: 22687441]
HepG2 2.2.15 IC50
1236.61 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as suppression of HbeAg secretion by ELISA
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as suppression of HbeAg secretion by ELISA
[PMID: 22472044]
HepG2 2.2.15 IC50
1238 μM
Compound: Tf
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of hepatitis B e antigen secretion by ELISA
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of hepatitis B e antigen secretion by ELISA
[PMID: 24731274]
HepG2 2.2.15 IC50
1389 μM
Compound: Tf
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of hepatitis B surface antigen secretion by ELISA
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of hepatitis B surface antigen secretion by ELISA
[PMID: 24731274]
HepG2 2.2.15 IC50
1446.35 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as suppression of HBsAg secretion by ELISA
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as suppression of HBsAg secretion by ELISA
[PMID: 22472044]
HepG2 2.2.15 IC50
1450.11 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral surface antigen secretion by ELISA
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral surface antigen secretion by ELISA
[PMID: 22687441]
HepG2 2.2.15 IC50
2.9 μM
Compound: Tenofovir
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as decrease in viral DNA replication treated for 7 days by real time PCR analysis
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as decrease in viral DNA replication treated for 7 days by real time PCR analysis
[PMID: 25737008]
HepG2 2.2.15 CC50
399 μM
Compound: Tenofovir
Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay
Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay
[PMID: 28082068]
HepG2 2.2.15 EC50
6.4 x 10-5 μM
Compound: TDF
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis
[PMID: 32421339]
HepG2 2.2.15 EC50
7.2 μM
Compound: PMPA, tenofovir
Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as viral DNA levels treated for 9 days measured after 24 hrs
Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as viral DNA levels treated for 9 days measured after 24 hrs
[PMID: 17646420]
Huh-7 EC50
4.2 μM
Compound: (R)-PMPA, Tenofovir
Antiviral activity against Hepatitis B virus infected in human HuH7 cells assessed as reduction in viral DNA level treated day 3 to day 8 post transfection by real time quantitative PCR analysis
Antiviral activity against Hepatitis B virus infected in human HuH7 cells assessed as reduction in viral DNA level treated day 3 to day 8 post transfection by real time quantitative PCR analysis
[PMID: 21803462]
L1210 IC50
11 μM
Compound: 2, (R)-PMPA
Cytostatic activity against mouse L1210 cells after 48 hrs by coulter counting analysis
Cytostatic activity against mouse L1210 cells after 48 hrs by coulter counting analysis
[PMID: 24686012]
MT2 CC50
> 100 μM
Compound: TFV
Cytotoxicity against human MT2 cells assessed as cell viability by CellTiter Glo assay
Cytotoxicity against human MT2 cells assessed as cell viability by CellTiter Glo assay
[PMID: 34549952]
MT2 CC50
> 1000 μM
Compound: 1, PMPA
Cytotoxicity against human MT2 cells after 5 days
Cytotoxicity against human MT2 cells after 5 days
[PMID: 19179082]
MT2 CC50
> 50000 nM
Compound: 2, PMPA or TFV
Cytotoxicity against human MT2 cells after 5 days by XTT assay
Cytotoxicity against human MT2 cells after 5 days by XTT assay
[PMID: 20409721]
MT2 EC50
0.65 μM
Compound: PMPA, tenofovir
Antiviral activity against HIV1 LAI in human MT2 cells assessed as inhibition of p24 antigen production by ELISA
Antiviral activity against HIV1 LAI in human MT2 cells assessed as inhibition of p24 antigen production by ELISA
[PMID: 17646420]
MT2 EC50
13 nM
Compound: 2, PMPA or TFV
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by XTT assay
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by XTT assay
[PMID: 20409721]
MT2 EC50
3.6 μM
Compound: 1, PMPA
Antiviral activity against HIV1 3a infected human MT2 cells assessed as inhibition of viral-induced cytopathic effect after 3 days by XTT assay
Antiviral activity against HIV1 3a infected human MT2 cells assessed as inhibition of viral-induced cytopathic effect after 3 days by XTT assay
[PMID: 19179082]
MT2 EC50
3.6 μM
Compound: 2
Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days
Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days
[PMID: 17562366]
MT2 EC50
5 μM
Compound: Tenofovir
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathic effect after 5 days by XTT assay
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathic effect after 5 days by XTT assay
[PMID: 27748590]
MT4 CC50
> 20 μM
Compound: PMPA
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 6 days by XTT tetrazolium dye-based assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 6 days by XTT tetrazolium dye-based assay
[PMID: 28682067]
MT4 EC50
0 μM
Compound: TDF
Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay
Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay
[PMID: 17548498]
PBMC CC50
> 100 μM
Compound: (R)-PMPA, Tenofovir
Cytotoxicity against PAP-activated human PBMC on day 7 by MTT assay
Cytotoxicity against PAP-activated human PBMC on day 7 by MTT assay
[PMID: 21803462]
PBMC CC50
> 100 μM
Compound: TFV
Cytotoxicity in uninfected human PBMC assessed as reduction in cell viability by XTT assay
Cytotoxicity in uninfected human PBMC assessed as reduction in cell viability by XTT assay
[PMID: 27933889]
PBMC CC50
> 100 μM
Compound: TFV
Cytotoxicity against human PBMC assessed as reduction in cell viability by XTT assay
Cytotoxicity against human PBMC assessed as reduction in cell viability by XTT assay
[PMID: 27405794]
PBMC CC50
> 25 μM
Compound: PMPA
Cytotoxicity against human PHA-stimulated PBMC assessed as cell viability by tetrazolium dye assay
Cytotoxicity against human PHA-stimulated PBMC assessed as cell viability by tetrazolium dye assay
[PMID: 28682067]
PBMC CC50
≥ 10 μM
Compound: (R)-PMPA; Tenofovir
Cytotoxicity against human PBMC assessed as reduction in cell growth after 7 days by MTT assay
Cytotoxicity against human PBMC assessed as reduction in cell growth after 7 days by MTT assay
[PMID: 29558735]
PBMC CC50
1270 μM
Compound: PMPA, tenofovir
Cytotoxicity against human PBMC by XTT assay
Cytotoxicity against human PBMC by XTT assay
[PMID: 17646420]
PBMC CC50
53 μM
Compound: TDF
Cytotoxicity against human PHA-PBMC cells by MTT assay
Cytotoxicity against human PHA-PBMC cells by MTT assay
[PMID: 17548498]
TZM CC50
> 100 μM
Compound: PMPA
Cytotoxicity against human TZM-bl cells assessed as cell viability by tetrazolium dye assay
Cytotoxicity against human TZM-bl cells assessed as cell viability by tetrazolium dye assay
[PMID: 28682067]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

287.21

Formula

C9H14N5O4P

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H](OCP(O)(O)=O)CN1C=NC2=C(N)N=CN=C12

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 7.69 mg/mL (26.77 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 2 mg/mL (6.96 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4818 mL 17.4089 mL 34.8177 mL
5 mM 0.6964 mL 3.4818 mL 6.9635 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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V1

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.77 mg/mL (2.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.77 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.77 mg/mL (2.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.77 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 1.96 mg/mL (6.82 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

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(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.89%

References
Cell Assay
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

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[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.4818 mL 17.4089 mL 34.8177 mL 87.0443 mL
5 mM 0.6964 mL 3.4818 mL 6.9635 mL 17.4089 mL
DMSO 10 mM 0.3482 mL 1.7409 mL 3.4818 mL 8.7044 mL
15 mM 0.2321 mL 1.1606 mL 2.3212 mL 5.8030 mL
20 mM 0.1741 mL 0.8704 mL 1.7409 mL 4.3522 mL
25 mM 0.1393 mL 0.6964 mL 1.3927 mL 3.4818 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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