|(6S,9S,9aS)-N-苄基-6-(4-羟基苄基)-2,9-二甲基-4,7-二氧代-8-(喹啉-8-基甲基)八氢-1H-吡嗪并[2,1-c][1,2,4]三嗪-1-甲酰胺|CsnPharm

CAS No.: 1422253-37-9

(6S,9S,9aS)-N-Benzyl-6-(4-hydroxybenzyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide Catalog No. CSN22363

C-82 is an active metabolite of PRI-724 which selectively inhibits the CBP/β-catenin interaction.

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技术信息

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 ... more >> Chicago, Illinois, United States United States, Massachusetts Boston, Massachusetts, United States United States, New York New York, New York, United States Collapse <<
NCT02432027	Psoriasis	Phase 1 Phase 2	Completed	-	Germany ... more >> Schwerin, Germany Collapse <<

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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7281 mL
- 8.6406 mL
- 17.2813 mL
- 5 mM
- 0.3456 mL
- 1.7281 mL
- 3.4563 mL
- 10 mM
- 0.1728 mL
- 0.8641 mL
- 1.7281 mL

技术信息

CAS号

1422253-37-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H34N6O4

运输

蓝冰

分子量

578.66

别名

溶解度

DMSO	120.0 mg/mL (207.4 mM)

动物实验配方

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(6S,9S,9aS)-N-Benzyl-6-(4-hydroxybenzyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide Catalog No. CSN22363

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