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

Tenofovir  (Synonyms: 替諾福韋; GS 1278; PMPA)

目錄號: HY-13910 純度: 99.89%
COA 產品使用指南

Tenofovir (GS 1278) 是一種核苷酸逆轉錄酶 (nucleotide reverse transcriptase) 抑制劑,可用于 HIV和慢性乙型肝炎 (Hepatitis B; HBV) 的研究。

MCE 的所有產品僅用作科學研究或藥證申報,我們不為任何個人用途提供產品和服務

Tenofovir Chemical Structure

Tenofovir Chemical Structure

CAS No. : 147127-20-6

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Other Forms of Tenofovir:

查看 HIV 亞型特異性產品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產品資料

  • 參考文獻

生物活性

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

IC50 & Target

HIV-1

 

細胞效力
(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]
體外研究
(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].

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

體內研究
(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].

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

Clinical Trial
分子量

287.21

Formula

C9H14N5O4P

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

替諾福韋;替洛福韋

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數據
細胞實驗: 

DMSO 中的溶解度 : 7.69 mg/mL (26.77 mM; 超聲助溶 (<80°C); 吸濕的 DMSO 對產品的溶解度有顯著影響,請使用新開封的 DMSO)

H2O 中的溶解度 : 2 mg/mL (6.96 mM; 超聲助溶)

配制儲備液
濃度 溶劑體積 質量 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
查看完整儲備液配制表

* 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內使用, -20°C儲存時,請在1年內使用。

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗:

請根據您的 實驗動物和給藥方式 選擇適當的溶解方案。

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結果的可靠性,澄清的儲備液可以根據儲存條件,適當保存;體內實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.77 mg/mL (2.68 mM); 澄清溶液

    此方案可獲得 ≥ 0.77 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 7.7 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.77 mg/mL (2.68 mM); 澄清溶液

    此方案可獲得 ≥ 0.77 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 7.7 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。

以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑: PBS

    Solubility: 1.96 mg/mL (6.82 mM); 澄清溶液; 超聲助溶 (<60°C)

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數量

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網站選購。 ,Tween 80,均可在 MCE 網站選購。
計算結果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲備液濃度超過該產品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術支持聯(lián)系。
動物實驗體內工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水
連續(xù)給藥周期超過半月以上,請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產品資料

純度: 99.89%

參考文獻
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.

參考文獻

完整儲備液配制表

* 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內使用, -20°C儲存時,請在1年內使用。

可選溶劑 濃度 溶劑體積 質量 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

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

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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Tenofovir
目錄號:
HY-13910
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