Capravirine
Capravirine (S-1153) is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) with potent antiviral activity. Capravirine inhibits replication of HIV-1 strains that are resistant to nucleoside/nucleotide reverse transcriptase inhibitors and other NNRTIs. Capravirine is metabolized by the cytochrome P450 enzyme CYP3A4.
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- CAS No.: 178979-85-6
- Formule: C20H20Cl2N4O2S
- Masse moléculaire:451.37
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MT2 | EC50 |
0.2 nM
Compound: CPV
|
Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS
Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS
|
[PMID: 19104010] |
| SUP-T1 | IC50 |
1.4 nM
Compound: Capravirine
|
Antiviral activity against HIV RF infected in human SupT1 cells
Antiviral activity against HIV RF infected in human SupT1 cells
|
[PMID: 19748778] |
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 178979-85-6
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Masse moléculaire 451.37
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Formule C20H20Cl2N4O2S
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SMILES
O=C(N)OCC1=NC(C(C)C)=C(N1CC2=CC=NC=C2)SC3=CC(Cl)=CC(Cl)=C3
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Synonyms
S-1153
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Pureté et documentation
Références
[1]. Bu HZ, et al. Metabolism and excretion of capravirine, a new non-nucleoside reverse transcriptase inhibitor, alone and in combination with ritonavir in healthy volunteers. Drug Metab Dispos. 2004 Jul;32(7):689-98. [Content Brief]
[2]. Gewurz BE, et al. Capravirine, a nonnucleoside reverse-transcriptase inhibitor in patients infected with HIV-1: a phase 1 study. J Infect Dis. 2004 Dec 1;190(11):1957-61. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)