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C-82

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Chemical Structure| 1422253-37-9 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
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

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

[1]Osawa Y, Oboki K, Imamura J, Kojika E, Hayashi Y, Hishima T, Saibara T, Shibasaki F, Kohara M, Kimura K. Inhibition of Cyclic Adenosine Monophosphate (cAMP)-response Element-binding Protein (CREB)-binding Protein (CBP)/β-Catenin Reduces Liver Fibrosis in Mice. EBioMedicine. 2015 Oct 8;2(11):1751-8. doi: 10.1016/j.ebiom.2015.10.010