Tivirapine
Tivirapine (R86183) is a nonnucleoside HIV-1 RT inhibitor against HIV-1-induced cytopathic effects with an EC50 value of 4 nM. Tivirapine inhibits the Yl8lC mutant of HIV-1 RT.
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- CAS No.: 137332-54-8
- 화학식: C16H20ClN3S
- 분자량:321.87
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| C8166 | CC50 |
50 μM
Compound: 8-CITIBO
|
Cytotoxicity against C8166 cells by MTT assay
Cytotoxicity against C8166 cells by MTT assay
|
[PMID: 16279773] |
| C8166 | EC50 |
0.03 μM
Compound: 8-ClTIBO
|
Antiviral activity against HIV1 3B infected human C8166 cells assessed as inhibition of syncytia formation by p24 antigen based assay
Antiviral activity against HIV1 3B infected human C8166 cells assessed as inhibition of syncytia formation by p24 antigen based assay
|
[PMID: 19170521] |
| C8166 | EC50 |
0.03 μM
Compound: 2 (8-CITIBO)
|
Concentration which produces a 50% survival of HIV-1 infected cells relative to uninfected control C8166 cells
Concentration which produces a 50% survival of HIV-1 infected cells relative to uninfected control C8166 cells
|
[PMID: 11462972] |
| C8166 | EC50 |
0.03 μM
Compound: 8-CITIBO
|
Inhibition of HIV1-3B replication in C8166 cells
Inhibition of HIV1-3B replication in C8166 cells
|
[PMID: 16279773] |
| C8166 | IC50 |
50 μM
Compound: 2 (8-CITIBO)
|
Concentration which results in 50% survival of uninfected untreated control C8166 cells (cytotoxicity of the compound)
Concentration which results in 50% survival of uninfected untreated control C8166 cells (cytotoxicity of the compound)
|
[PMID: 11462972] |
| MT2 | EC50 |
14 nM
Compound: 2, 8-Cl-TIBO
|
Antiviral activity against HIV-1 infected un MT2 cells assessed as virus-induced cytopathicity after 5 days by MTT assay
Antiviral activity against HIV-1 infected un MT2 cells assessed as virus-induced cytopathicity after 5 days by MTT assay
|
[PMID: 23380374] |
| MT2 | IC50 |
>100 nM
Compound: 2, 8-Cl-TIBO
|
Cytotoxicity against human MT2 cells after 5 days by MTT assay
Cytotoxicity against human MT2 cells after 5 days by MTT assay
|
[PMID: 23380374] |
| MT4 | EC50 |
0.0043 μM
Compound: 9, R86183
|
Antiviral activity against Human immunodeficiency virus 1 infected in human MT4 cells
Antiviral activity against Human immunodeficiency virus 1 infected in human MT4 cells
|
[PMID: 19632850] |
| MT4 | EC50 |
4.6 nM
Compound: 3
|
Effective concentration of the compound to inhibit HIV-1 replication in HIV-infected MT-4 cells
Effective concentration of the compound to inhibit HIV-1 replication in HIV-infected MT-4 cells
|
[PMID: 15771411] |
| MT4 | IC50 |
0.0043 μM
Compound: 6a
|
Concentration required for 50% protection of MT-4 cells against the cytopathic effect of HIV-1
Concentration required for 50% protection of MT-4 cells against the cytopathic effect of HIV-1
|
[PMID: 7877144] |
Chemical Information
-
CAS No. 137332-54-8
-
분자량 321.87
-
화학식 C16H20ClN3S
-
SMILES
ClC(C1=C2N3C[C@@H](N(C1)C/C=C(C)\C)C)=CC=C2NC3=S
-
Synonyms
R86183; TIBO R 86183
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Ding J, et al. Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors. Nat Struct Biol. 1995 May;2(5):407-15. [Content Brief]
[2]. Zhou Z, et al. Relative free energy of binding and binding mode calculations of HIV-1 RT inhibitors based on dock-MM-PB/GS. Proteins. 2004 Nov 15;57(3):493-503. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)