product name
γ分泌酶抑制剂 XX, This γ-secretase inhibitor, CAS 209984-56-5, is a cell-permeable dibenzazepine compound that lowers both brain and plasma Aβ40 levels by ~72% in Tg2576 mutant APP transgenic mouse model.
质量水平
检测方案
≥95% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white
溶解性
DMSO: 10 mg/mL
运输
ambient
储存温度
−20°C
InChI
1S/C26H23F2N3O3/c1-15(29-23(32)13-16-11-17(27)14-18(28)12-16)25(33)30-24-21-9-4-3-7-19(21)20-8-5-6-10-22(20)31(2)26(24)34/h3-12,14-15,24H,13H2,1-2H3,(H,29,32)(H,30,33)/t15-,24-/m0/s1
InChI key
QSHGISMANBKLQL-OWJWWREXSA-N
一般描述
一种细胞渗透性二苯并氮杂（dbz）化合物，可作为有效的γ-分泌酶抑制剂，在Tg2576突变APP转基因小鼠模型（100 µmol/kg, b.i.d）中，显著降低脑和血浆Aβ40水平，约72%。诱导肠道中隐窝结构增殖单位和结肠干细胞生态位的异质重组。在C57BL/6和ApcMin小鼠模型（10 µmol/kg，i.p.）中，还可能抑制Notch加工（在SupT1细胞中IC50 = 1.7 nM），并诱导增殖隐窝细胞转化为有丝分裂后杯状细胞。
一种细胞渗透性有效γ-分泌酶抑制剂，在Tg2576突变APP转基因小鼠模型（100 µmol/kg，b.i.d.）中可显著降低脑和血浆Aβ40水平，约72%。诱导肠道中隐窝结构增殖单位和结肠干细胞生态位的异质重组。在C57BL/6和ApcMin小鼠模型（10 µmol/kg，i.p.）中，还可能抑制Notch加工（在SupT1细胞中IC50 = 1.7 nM），并诱导增殖隐窝细胞转化为有丝分裂后杯状细胞。
生化/生理作用
产物不与ATP竞争。
可逆：否
细胞可渗透性：是
靶标IC50：1.7 nM抑制SupT1细胞中的Notch加工
包装
用惰性气体包装
警告
毒性：标准处理（A）
其他说明
Droy-Dupré, L., et al. 2012.Dis.Model Mech.5, 107.
van Es, J.H., et al. 2005.Nature435, 959.
Milano, J., et al. 2004.Toxicol.Sci.82, 341.
van Es, J.H., et al. 2005.Nature435, 959.
Milano, J., et al. 2004.Toxicol.Sci.82, 341.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral - Skin Sens. 1A
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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