GS-9148
GS-9148 is a ribose-modified HIV-1 nucleotide reverse transcriptase (RT) inhibitor with an EC50 value of 10.6 µM. GS-9148 shows antiretroviral activity for K65R, L74V, or M184V RT mutation.
For research use only. We do not sell to patients.
- CAS No.: 875608-25-6
- Formula: C10H11FN5O5P
- Molecular Weight:331.20
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | CC50 |
182 μM
Compound: GS-9148
|
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 |
≥4.5 μM
Compound: GS-9148
|
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 |
≥95 μM
Compound: GS-9148
|
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] |
| MT2 | EC50 |
12.3 μM
Compound: 1, GS-9148, 2'-Fd4AP
|
Antiviral activity against HIV1 3B in MT2 cells
Antiviral activity against HIV1 3B in MT2 cells
|
[PMID: 18082402] |
| MT2 | CC50 |
>1000 μM
Compound: 1, GS-9148, 2'-Fd4AP
|
Cytotoxicity against human MT2 cells
Cytotoxicity against human MT2 cells
|
[PMID: 18082402] |
| MT2 | EC50 |
12.3 μM
Compound: 4, 2'-Fd4AP
|
Antiviral activity against wild type HIV1 3B in MT2 cells
Antiviral activity against wild type HIV1 3B in MT2 cells
|
[PMID: 18164198] |
| MT2 | IC50 |
1.9 μM
Compound: 4, 2'-Fd4AP
|
Inhibition of wild type HIV 3B reverse transcriptase in MT2 cells
Inhibition of wild type HIV 3B reverse transcriptase in MT2 cells
|
[PMID: 18164198] |
| MT2 | CC50 |
>1000 μM
Compound: 4, 2'-Fd4AP
|
Cytotoxicity against human MT2 cells
Cytotoxicity against human MT2 cells
|
[PMID: 18164198] |
| MT2 | EC50 |
12 μM
Compound: 3, GS-9148
|
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 | CC50 |
>1000 μM
Compound: 3, GS-9148
|
Cytotoxicity against human MT2 cells after 5 days
Cytotoxicity against human MT2 cells after 5 days
|
[PMID: 19179082] |
| MT2 | EC50 |
10600 nM
Compound: 4, 2'-Fd4AP, GS-9148
|
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 | CC50 |
>100000 nM
Compound: 4, 2'-Fd4AP, GS-9148
|
Cytotoxicity against human MT2 cells after 5 days by XTT assay
Cytotoxicity against human MT2 cells after 5 days by XTT assay
|
[PMID: 20409721] |
Chemical Information
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CAS No. 875608-25-6
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Molecular Weight 331.20
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Formula C10H11FN5O5P
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SMILES
OP(O)(CO[C@H]1O[C@H](C(F)=C1)N2C=NC3=C(N=CN=C23)N)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)