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Cat.No.S1401
| Related Targets | Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite HIV HCV Protease |
|---|---|
| Other Reverse Transcriptase Products | Dapivirine (TMC120) Salicylanilide Fangchinoline Bifendate 3'-Fluoro-3'-deoxythymidine (Alovudine) Ulonivirine Lersivirine (UK-453061) 4-Chloro-2-(trifluoroacetyl)aniline hydrochloride |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| human MT2 cells | Function assay | 5 days | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by XTT assay, EC50=0.013 μM | |||
| human H9 cells | Function assay | Antiviral activity against HIV1 clade F isolate 2338 infected in human H9 cells assessed as inhibition of viral replication, EC50=0.04 μM | ||||
| C3H/3T3 cells | Function assay | 6 days | Inhibition of murine sarcoma virus-induced transformation of mouse embryo fibroblast C3H/3T3 cells after 6 days, EC50=0.23 μM | |||
| CEM (human leukemia) cells | Function assay | Antiviral activity against HIV-1 (IIIB) in CEM (human leukemia) cells, EC50=1.2 μM | ||||
| MT-4 cells | Function assay | In vitro antiviral activity against HIV-2 in MT-4 cells, EC50=1.4 μM | ||||
| human bone marrow cells | Cytotoxicity assay | 24 h | Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay, CC50=3.5 μM | |||
| C8166 cells | Function assay | 4 days | 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, EC50=7.1 μM | |||
| mouse L1210 cells | Cytotoxicity assay | 48 h | Cytostatic activity against mouse L1210 cells after 48 hrs by coulter counting analysis, IC50=11 μM | |||
| human HepG2 cells | Function assay | 9 days | Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay, IC50=12.3 μM | |||
| human HeLa cells | Cytotoxicity assay | 72 h | Cytostatic activity against human HeLa cells after 72 hrs by coulter counting analysis, IC50=17 μM | |||
| CHO cells | Cytotoxicity assay | 120 h | Cytotoxicity against CHO cells after 120 hrs by Cell-Titer Glo assay, CC50=21 μM | |||
| MDCK2 cells | Function assay | 10 μM | Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay | |||
| human HepG2 cells | Cytotoxicity assay | 14 days | Cytotoxicity against human HepG2 cells assessed as inhibition of cellular DNA replication after 14 days | |||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 4 mg/mL
(13.92 mM)
Water : 2 mg/mL Ethanol : Insoluble |
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In vivo |
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| Molecular Weight | 287.21 | Formula | C9H14N5O4P |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 147127-20-6 | Download SDF | Storage of Stock Solutions |
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| Synonyms | GS-1278 | Smiles | CC(CN1C=NC2=C(N=CN=C21)N)OCP(=O)(O)O | ||
| Features |
Tenofovir disoproxil fumarate is the prodrug form of tenofovir.
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| Targets/IC50/Ki |
Reverse transcriptase
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| In vitro |
Tenofovir 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. This compound also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). It is uniquely active against multinucleoside-resistant HIV expressing the Q151M mutation, but shows reduced susceptibility to the T69S insertion mutations. This chemical inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells. It (4 μM) completely inhibits the growth of HIVIIIB in MT-2 cells. This compound inhibits synthesis of negative strand strong-stop DNA with IC50 of 9 µM for wild-type RT, 6 µM for M184V RT and 50 µM for K65R RT.
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| In vivo |
Tenofovir (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. This compound 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. It completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques.
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References |
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