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Merck
CN

565789

γ分泌酶抑制剂 XX

≥95% (HPLC), solid, γ-secretase inhibitor, Calbiochem®

别名:

γ分泌酶抑制剂 XX, （S，S）-2-[2-（3,5-二氟苯基）乙酰氨基]-N-（5-甲基-6-氧代-6,7-二氢-5H-二苯并[b，d]氮杂卓-7-基）丙酰胺，DBZ，二苯并氮卓

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关于此项目

经验公式（希尔记法）:
C26H23F2N3O3
化学文摘社编号:
209984-56-5
分子量:
463.48
MDL number:
MFCD12828734
UNSPSC Code:
12352200
NACRES:
NA.77

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产品名称

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.

SMILES string

Fc1cc(cc(c1)CC(=O)N[C@@H](C)C(=O)N[C@H]2c3c(cccc3)c4c(cccc4)N(C2=O)C)F

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

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

相关类别

Biochem/physiol Actions

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

Disclaimer

毒性：标准处理（A）

General description

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。

Other Notes

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.

Packaging

用惰性气体包装

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302,H317

Hazard Classifications

Acute Tox. 4 Oral - Skin Sens. 1A

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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