产品
编 号：F290283
分子式：C20H19N5
分子量：329.4
分子式：C20H19N5
分子量：329.4
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规格
价格
是否有货
10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 244767-67-7
产品详情
生物活性：
Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.
体内研究：
Dapivirine (16 mg/kg, once every 3 days for 12 days) exhibits potent antitumor activity in human glioblastoma models in mice.Dapivirine has been shown to have a half-life in the range of 65 to 90 h.Animal Model:U87 cells were subcutaneously injected into the nude mice.
Dosage:16 mg/kg.
Administration:Once every 3 days for 12 days.
Result:Significantly decreased the tumor volumes.A significant decrease in Ki67 (a marker for proliferating cells that is overexpressed in many cancers) staining in sections of dapivirine-treated tumors compared to tumors from vehicle-treated mice.
体外研究：
Dapivirine (4-64 μM, 24, 48, 72, 96 and 120 hours) inhibits proliferation of glioma cells and induces apoptosis (16 μM, 12-48 h).Dapivirine (8 and 16 μM, 12 h) enhances invasion of glioma cells.Dapivirine (16 μM, 12 h, 24 h and 48 h) promotes autophagy in U87 cells.Dapivirine(TMC120-R147681) apparently blocks infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration.
Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.
体内研究：
Dapivirine (16 mg/kg, once every 3 days for 12 days) exhibits potent antitumor activity in human glioblastoma models in mice.Dapivirine has been shown to have a half-life in the range of 65 to 90 h.Animal Model:U87 cells were subcutaneously injected into the nude mice.
Dosage:16 mg/kg.
Administration:Once every 3 days for 12 days.
Result:Significantly decreased the tumor volumes.A significant decrease in Ki67 (a marker for proliferating cells that is overexpressed in many cancers) staining in sections of dapivirine-treated tumors compared to tumors from vehicle-treated mice.
体外研究：
Dapivirine (4-64 μM, 24, 48, 72, 96 and 120 hours) inhibits proliferation of glioma cells and induces apoptosis (16 μM, 12-48 h).Dapivirine (8 and 16 μM, 12 h) enhances invasion of glioma cells.Dapivirine (16 μM, 12 h, 24 h and 48 h) promotes autophagy in U87 cells.Dapivirine(TMC120-R147681) apparently blocks infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration.
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