C-82
产品说明书
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同义名 : | - |
| CAS号 : | 1422253-37-9 | |
| 货号 : | A329844 | |
| 分子式 : | C33H34N6O4 | |
| 纯度 : | 99%+ | |
| 分子量 : | 578.661 | |
| MDL号 : | MFCD32664545 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The cAMP-response element-binding protein-binding protein (CBP)/β-catenin-mediated transcription is essential for cell proliferation and non-differentiation, and is implicated in liver fibrosis. C-82 (the active form of PRI-724) is a second-generation CBP/β-catenin antagonist that inhibits the binding between CBP and β-catenin and increases the binding between β-catenin and p300. C-82 at a concentration of 10μM inhibited the β-catenin signaling in isolated mouse primary quiescent hepatic stellate cells (HSCs) during activation, while the removal of C-82 rapidly restored the features of HSC activation. C-82 treatment also inhibited most gene upregulation induced by HSC activation. Three-day treatment with C-82 (10μM) decreased the mRNA expression of fibrosis-related makers in activated HSCs. Cells started to death seven days following C-82 administration. C-82 treatment also decreased the mRNA expression of survivin, a factor that protects fibroblasts from apoptosis, in activated HSCs. However, C-82 did not induce cell death in quiescent HSCs for at least 15 days. Co-administration of PRI-724 (0.4mg/mouse, four times a week) for 4 weeks reduced CCL4-induced liver fibrosis in C57BL/6 male mice (6 – 9 month-old).[1] | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02349009 | Systemic Scleroderma | Phase 1 Phase 2 | Completed | - | United States, Illinois ... 展开 >> Chicago, Illinois, United States United States, Massachusetts Boston, Massachusetts, United States United States, New York New York, New York, United States 收起 << |
| NCT02432027 | Psoriasis | Phase 1 Phase 2 | Completed | - | Germany ... 展开 >> Schwerin, Germany 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.73mL 0.35mL 0.17mL |
8.64mL 1.73mL 0.86mL |
17.28mL 3.46mL 1.73mL |
| 参考文献 |
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