Structure of Tenofovir hydrate
CAS No.: 206184-49-8
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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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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 |
GHS Pictogram: |
![]() |
Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H332-H335 |
Precautionary Statements: | P280-P305+P351+P338-P310 |
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 << |
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 |
Tags: Tenofovir | GS 1278 | PMPA | GS1278 | GS-1278 | HIV | Reverse Transcriptase | Human immunodeficiency virus | HIV-1 IIIB | HIV-2 ROD | HIV-1 (IIIB) | HIV-2(ROD)Tenofovir hydrate | GS 1278 hydrate | nucleotide reverse transcriptase inhibitor | NRTI | reverse transcriptase inhibition | viral DNA chain termination | chronic hepatitis B | HIV replication blockade | 206184-49-8
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H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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