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Merck

565789

γ-Secretase Inhibitor XX

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

別名:

γ-Secretase Inhibitor XX, (S,S)-2-[2-(3,5-Difluorophenyl)acetylamino]-N-(5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propionamide, DBZ, Dibenzazepine

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この商品について

実験式(ヒル表記法):
C26H23F2N3O3
CAS番号:
分子量:
463.48
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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製品名

γ-Secretase Inhibitor 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

Biochem/physiol Actions

Cell permeable: yes
Product does not compete with ATP.
Reversible: no
Target IC50: 1.7 nM inhibiting Notch processing in SupT1 cells

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable dibenzazepine (dbz) compound that acts as a potent γ-secretase inhibitor and significantly lowers both brain and plasma Aβ40 levels by ~72% in Tg2576 mutant APP transgenic mouse model (100 µmol/kg, b.i.d). Induces a heterogeneous reorganization of the crypt structural-proliferative units in the intestinal tract and of the stem cell niche in the colon. Also potently inhibits Notch processing (IC50 = 1.7 nM in SupT1 cells) and induces conversion of proliferative crypt cells to post-mitotic goblet cells in both the C57BL/6 and ApcMin mouse models (10 µmol/kg, i.p).
A cell-permeable, potent γ-secretase inhibitor that significantly lowers both brain and plasma Aβ40 levels by ~72% in Tg2576 mutant APP transgenic mouse model (100 µmol/kg, b.i.d). Induces a heterogeneous reorganization of the crypt structural-proliferative units in the intestinal tract and of the stem cell niche in the colon. Also potently inhibits Notch processing (IC50 = 1.7 nM in SupT1 cells) and induces conversion of proliferative crypt cells to post-mitotic goblet cells in both the C57BL/6 and ApcMin mouse models (10 µmol/kg, i.p).

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

Packaged under inert gas

Legal Information

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

pictograms

Exclamation mark

signalword

Warning

hcodes

Hazard Classifications

Acute Tox. 4 Oral - Skin Sens. 1A

保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


試験成績書(COA)

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文書ライブラリにアクセスする

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eLife, 12 (2024-01-05)
The unlimited expansion of human progenitor cells in vitro could unlock many prospects for regenerative medicine. However, it remains an important challenge as it requires the decoupling of the mechanisms supporting progenitor self-renewal and expansion from those mechanisms promoting their
Lina Sui et al.
Current protocols in human genetics, 99(1), e68-e68 (2018-09-08)
Insulin-expressing beta cells are crucial for the maintenance of systemic glucose homeostasis. Elucidation of the molecular and cellular mechanisms of beta cell development, expansion, survival, and function are required for full understanding of the molecular pathogenesis of diabetes. However, access
Luiza Ghila et al.
Methods in molecular biology (Clifton, N.J.), 2454, 327-349 (2021-04-01)
Pancreatic islet endocrine cells generated from patient-derived induced pluripotent stem cells represent a great strategy for both disease modeling and regenerative medicine. Nevertheless, these cells inherently miss the effects of the intricate network of systemic signals characterizing the living organisms.
ZnT8 Loss of Function Mutation Increases Resistance of Human Embryonic Stem Cell-Derived Beta Cells to Apoptosis in Low Zinc Condition.
Sui, et al.
Cells, 12 (2023)
Anup K Nair et al.
Cells, 11(9) (2022-05-15)
The top genetic association signal for type 2 diabetes (T2D) in Southwestern American Indians maps to intron 15 of KCNQ1, an imprinted gene. We aim to understand the biology whereby variation at this locus affects T2D specifically in this genomic

グローバルトレードアイテム番号

カタログ番号GTIN
565789-500UGCN04055977191844
565789-1MGCN04055977191837

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