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Chemical Structure| 206184-49-8 Chemical Structure| 206184-49-8

Structure of Tenofovir hydrate
CAS No.: 206184-49-8

Chemical Structure| 206184-49-8

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Tenofovir is a nucleotide analogue reverse transcriptase inhibitors (NRTIs) which reduces the viral cytopathic effect of HIV-1 (IIIB), HIV-2(ROD) with EC50 of 1.15 μg/ml and 1.12 μg/ml.

Synonyms: PMPA hydrate; GS 1278 hydrate

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Product Details of Tenofovir hydrate

CAS No. :206184-49-8
Formula : C9H16N5O5P
M.W : 305.23
SMILES Code : NC1=NC=NC2=C1N=CN2C[C@H](OCP(O)(O)=O)C.[H]O[H]
Synonyms :
PMPA hydrate; GS 1278 hydrate
MDL No. :MFCD11519982
InChI Key :PINIEAOMWQJGBW-FYZOBXCZSA-N
Pubchem ID :21146529

Safety of Tenofovir hydrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P280-P305+P351+P338-P310

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MΦ cells 5-600 µg/mL 5 days Evaluate the cell viability of Tenofovir, AuNPs, and AuNP-TNF in MΦ cells, showing that the viability of AuNP-TNF-treated cells was significantly higher than those treated with free TNF. PMC9850711
PBMCs 5-600 µg/mL 5 days Evaluate the cell viability of Tenofovir, AuNPs, and AuNP-TNF in PBMCs, showing that the viability of AuNP-TNF-treated cells was significantly higher than those treated with free TNF. PMC9850711
TZM-bl cells 5-600 µg/mL 48 h Evaluate the cell viability of Tenofovir, AuNPs, and AuNP-TNF in TZM-bl cells, showing that the viability of AuNP-TNF-treated cells was significantly higher than those treated with free TNF. PMC9850711
CD4+ T cells 10 μM 12 h To stop ongoing HIV-1 infection, the results showed that Tenofovir effectively suppressed viral replication. PMC10907297
MΦ cells 5-600 µg/mL 5 days Assess cell viability, results showed that AuNP-TNF had significantly higher cell viability than free TNF. PMC9850711
PBMCs 5-600 µg/mL 5 days Assess cell viability, results showed that AuNP-TNF had significantly higher cell viability than free TNF. PMC9850711
TZM-bl cells 5-600 µg/mL 48 h Assess cell viability, results showed that AuNP-TNF had significantly higher cell viability than free TNF. PMC9850711
NL4.3-ΔNef-eGFP infected CD4+ T cells 10 μM 12 h To inhibit viral replication and prevent ongoing infection. The results showed that Tenofovir successfully inhibited viral replication, and no ongoing infection was observed in the experiment. PMC10907297
CD4+ T cells 10 μM 18 h To inhibit viral replication and prevent viral persistence in cells. The results showed that Tenofovir successfully inhibited viral replication, and no ongoing infection was observed in the experiment. PMC10907297

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MISTRG-6-15 mouse model Oral 1 g/kg Not specified Suppress HIV-1 replication PMC9753998
BALB/c mice Healthy mice Intravenous injection 5 mg/kg Single injection, observed for 7 days Evaluate the biodistribution of Cy5.5-AuNPs in BALB/c mice, showing that Cy5.5-AuNPs mainly accumulated in the liver and lungs, and gradually decreased within 7 days. PMC9850711
Mice Chronic unpredictable mild stress (CUMS) model Gastric administration 30 mg/kg Once daily for 2 weeks Tenofovir significantly reversed the chronic stress-induced negative emotional behaviors, including increased center time% in the open field test, increased open arms time% and open arms entries% in the elevated plus maze test, increased recognition index in the novel object recognition test, increased sucrose preference% in the sucrose preference test, and decreased immobility time% in both the forced swimming and tail suspension tests. PMC9933381
Mice BLT humanized mouse model Oral 1560 mg/kg Once daily for five weeks Tenofovir was used to suppress HIV infection, and ART successfully suppressed the virus to below the limit of detection PMC9975043
Mice Pregnant mice Oral gavage 100 mg/kg Once daily for 5 days Tenofovir treatment reduced red blood cell counts, bone marrow cellularity, splenic HSCs, and erythroid progenitor numbers in pregnant mice, and decreased HSC division rates. PMC11709122
Mice HIV infection model Oral 5.35mg Once daily for 42 days To evaluate the effect of antiretroviral therapy on HIV-infected mice PMC9732419
Rhesus macaques SIV infection model Intravenous infusion 0.1 mg/kg Weekly for 3 or 10 weeks To evaluate the latency reversal effect of AZD5582 in SIV-infected rhesus macaques, results showed that AZD5582 induced SIV-RNA expression. PMC7111210
Hu-NSG-Tg (IL-15) mice HIV infection model Intraperitoneal injection 500 µg/mouse Twice a week for 2 weeks To evaluate the antiviral effect of Bi-Ab32/16 in an HIV-infected mouse model. Results showed that Bi-Ab32/16 treatment led to a significant decline in NK cell numbers and was negatively correlated with the time to viral rebound, indicating potential adverse effects on NK cell dynamics. PMC11829058
Mice HIV-1 infection model Oral 1,560 mg/kg Daily until the end of the study To suppress HIV-1 replication, the results showed that Tenofovir effectively reduced viral load. PMC10907297
Mice BLT mouse model Oral 80 mg/kg Daily Evaluate the antiviral efficacy of Tenofovir in HIV-infected mice PMC11163220
Mice HIV-1 infection model Oral 90 mg/kg Daily for 7 weeks Suppress HIV-1 viral replication PMC10518630
Mice Chronic unpredictable mild stress (CUMS) model Gastric administration 30 mg/kg Once daily for 2 weeks Tenofovir significantly reversed chronic stress-induced negative emotional behaviors, including reduced anxiety- and depressive-like behaviors, and improved microglial morphological activation and biological immuno-inflammation. PMC9933381
NSG mice BLT humanized mouse model Oral 1,560mg/kg Continuous administration Evaluate the impact of Gal-9 on HIV persistence PMC9975043
Mice Pregnant and non-pregnant mice Oral gavage 100 mg/kg Daily for 5 days In non-pregnant female mice, reverse transcriptase inhibitors had little or no effect on blood cell counts, or bone marrow or spleen hematopoiesis. In pregnant mice, reverse transcriptase inhibitors reduced red blood cell counts, bone marrow cellularity and the frequency of HSCs and LSK cells in the spleen. The absolute number of CD71+Ter119+ erythroid progenitors declined in the spleens of pregnant mice treated with reverse transcriptase inhibitors. PMC11709122
Humanized DRAGA mice HIV infection model Oral 5.35mg Once daily for 42 days Evaluate the therapeutic effect of antiretroviral therapy on HIV infection PMC9732419
Hu-NSG-Tg (IL-15) mice HIV infection model Oral 131 mg/kg From 6 to 9 weeks post-infection (WPI) To evaluate the therapeutic effect of Tenofovir in an HIV infection model PMC11829058
Mice HIV infection model Oral 80 mg/kg Continuous administration Suppression of HIV replication PMC11163220
NSG mice Humanized mouse model of HIV-1 infection Oral 90 mg/kg Once daily for seven weeks Suppress HIV-1 viral replication PMC10518630

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01475851 Hepatitis B, Chronic Phase 3 Completed - Japan ... More >> GSK Investigational Site Aichi, Japan, 466-8560 GSK Investigational Site Aichi, Japan, 467-8602 GSK Investigational Site Chiba, Japan, 260-8677 GSK Investigational Site Fukuoka, Japan, 803-8505 GSK Investigational Site Hiroshima, Japan, 734-8551 GSK Investigational Site Hokkaido, Japan, 060-0033 GSK Investigational Site Kagoshima, Japan, 890-8520 GSK Investigational Site Kanagawa, Japan, 213-8587 GSK Investigational Site Miyagi, Japan, 980-8574 GSK Investigational Site Tokyo, Japan, 105-8470 GSK Investigational Site Tokyo, Japan, 180-8610 Less <<
NCT01475851 - Completed - -
NCT01480284 - Completed - -
NCT01480284 Hepatitis B, Chronic Phase 3 Completed - Japan ... More >> GSK Investigational Site Aichi, Japan, 466-8560 GSK Investigational Site Aichi, Japan, 467-8602 GSK Investigational Site Chiba, Japan, 260-8677 GSK Investigational Site Fukui, Japan, 918-8503 GSK Investigational Site Fukuoka, Japan, 803-8505 GSK Investigational Site Fukuoka, Japan, 810-8539 GSK Investigational Site Fukuoka, Japan, 812-8582 GSK Investigational Site Fukuoka, Japan, 820-8505 GSK Investigational Site Gifu, Japan, 500-8717 GSK Investigational Site Hiroshima, Japan, 734-8530 GSK Investigational Site Hyogo, Japan, 651-2273 GSK Investigational Site Hyogo, Japan, 663-8501 GSK Investigational Site Kagawa, Japan, 760-8557 GSK Investigational Site Kagoshima, Japan, 890-8520 GSK Investigational Site Kagoshima, Japan, 892-8512 GSK Investigational Site Kanagawa, Japan, 213-8587 GSK Investigational Site Kumamoto, Japan, 862-8655 GSK Investigational Site Miyagi, Japan, 980-8574 GSK Investigational Site Miyazaki, Japan, 880-0003 GSK Investigational Site Nagasaki, Japan, 852-8501 GSK Investigational Site Nagasaki, Japan, 856-8562 GSK Investigational Site Nara, Japan, 630-8305 GSK Investigational Site Okayama, Japan, 700-0913 GSK Investigational Site Okayama, Japan, 700-8511 GSK Investigational Site Osaka, Japan, 540-0006 GSK Investigational Site Osaka, Japan, 564-0013 GSK Investigational Site Saga, Japan, 840-8571 GSK Investigational Site Tokyo, Japan, 105-8470 GSK Investigational Site Tokyo, Japan, 105-8471 GSK Investigational Site Tokyo, Japan, 140-8522 GSK Investigational Site Tokyo, Japan, 162-8655 GSK Investigational Site Tokyo, Japan, 180-8610 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.28mL

0.66mL

0.33mL

16.38mL

3.28mL

1.64mL

32.76mL

6.55mL

3.28mL

References

 

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