R82913
R82913 (9-Cl-TIBO) is a potent and high selective inhibitor of HIV-1 reverse transcriptase with antiviral activity on both an RNA template (negative strand synthesis) and a DNA template (positive strand synthesis). R82913 inhibits the replication of different strains of HIV-I in CEM cells with a median IC50 value of of 0.15 μM.
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- CAS 番号: 126347-69-1
- 分子式: C16H20ClN3S
- 分子量:321.87
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C8166 | EC50 |
0.002 μM
Compound: 1c (R 82913)
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Inhibitory activity against HIV-111B in C8166 cells
Inhibitory activity against HIV-111B in C8166 cells
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10.1016/0960-894X(95)00203-6 |
| C8166 | CC50 |
34 μM
Compound: TIBO R-82913
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Cytotoxic activity was evaluated in CD4+ lymphoblastoid cell line
Cytotoxic activity was evaluated in CD4+ lymphoblastoid cell line
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10.1016/0960-894X(95)00257-T |
| C8166 | IC50 |
0.0015 μM
Compound: TIBO R-82913
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Antiviral activity was evaluated by inhibition of HIV-1 replication in CD4+ lymphoblastoid cell line infected with HIV/IIIB strain
Antiviral activity was evaluated by inhibition of HIV-1 replication in CD4+ lymphoblastoid cell line infected with HIV/IIIB strain
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10.1016/0960-894X(95)00257-T |
| C8166 | EC50 |
0.002 μM
Compound: R-82913
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Tested against HIV-1 111B for Inhibition of viral replication by determining reduction of syncytia formation and antigen gp120 in C8166 cells, estimated by ELISA
Tested against HIV-1 111B for Inhibition of viral replication by determining reduction of syncytia formation and antigen gp120 in C8166 cells, estimated by ELISA
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10.1016/S0960-894X(97)00022-X |
| CEM-SS | CC50 |
>10000 nM
Compound: TIBO R-82913
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Cytotoxicity against wild type HIV-1-IIIB strain infected CEMSS cells.
Cytotoxicity against wild type HIV-1-IIIB strain infected CEMSS cells.
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[PMID: 7473595] |
| CEM-SS | IC50 |
>10000 nM
Compound: TIBO R-82913
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Inhibition of wild type HIV-1-IIIB strain replication in CEM-SS cells
Inhibition of wild type HIV-1-IIIB strain replication in CEM-SS cells
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[PMID: 7473595] |
| CEM-SS | CC50 |
35 μM
Compound: R-82913
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Tested for the cytotoxicity against CEM-SS cells (determined by the inhibition of [3H]-thymidine uptake)
Tested for the cytotoxicity against CEM-SS cells (determined by the inhibition of [3H]-thymidine uptake)
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10.1016/S0960-894X(01)81224-5 |
| CEM-SS | IC50 |
0.055 μM
Compound: R-82913
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Tested for the inhibition of HIV-1 in CEM-SS cells measured using Syncytial assay
Tested for the inhibition of HIV-1 in CEM-SS cells measured using Syncytial assay
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10.1016/S0960-894X(01)81224-5 |
| MOLT-4 | IC50 |
0.19 μM
Compound: TIBO R-82913
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Anti-HIV activity against HIV-1 in Molt-4 cells using 7-day infective assay
Anti-HIV activity against HIV-1 in Molt-4 cells using 7-day infective assay
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[PMID: 7506311] |
| MOLT-4 | IC50 |
19 μM
Compound: TIBO R-82913
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Tested for cytotoxicity in Molt-4 cells by XTT assay
Tested for cytotoxicity in Molt-4 cells by XTT assay
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[PMID: 7506311] |
| MT4 | EC50 |
33 nM
Compound: 2
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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
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[PMID: 15771411] |
| MT4 | IC50 |
0.039 μM
Compound: 8b
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Ability to block replication of HIV-1 virus in mock infected MT-4 cells
Ability to block replication of HIV-1 virus in mock infected MT-4 cells
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[PMID: 1956037] |
| MT4 | IC50 |
0.034 μM
Compound: 1a
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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] |
| MT4 | IC50 |
0.042 μM
Compound: 2
|
Compound was tested for its anti HIV-1 activity in MT-4 cells.
Compound was tested for its anti HIV-1 activity in MT-4 cells.
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10.1016/S0960-894X(01)80460-1 |
化学情報
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CAS 番号 126347-69-1
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分子量 321.87
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分子式 C16H20ClN3S
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SMILES
S=C1N2C3=C(C=C(C=C3N1)Cl)CN([C@H](C2)C)C/C=C(C)\C
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別名
9-Cl-TIBO
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. White EL, et al. A TIBO derivative, R82913, is a potent inhibitor of HIV-1 reverse transcriptase with heteropolymer templates. Antiviral Res. 1991 Oct;16(3):257-66. [Content Brief]
[2]. Larder BA. 3'-Azido-3'-deoxythymidine resistance suppressed by a mutation conferring human immunodeficiency virus type 1 resistance to nonnucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother. 1992 Dec;36(12):2664-9. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)