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565789

γ-Secretase Inhibitor XX

Name: &#947;-Secretase Inhibitor XX
Brand: MM

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

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):

C₂₆H₂₃F₂N₃O₃

CAS Number:

209984-56-5

Molecular Weight:

463.48

MDL number:

MFCD12828734

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥95% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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Properties

Product Name

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.

Quality Segment

100

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

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

Description

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 Apc^Min 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 Apc^Min mouse models (10 µmol/kg, i.p).

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

Packaging

Packaged under inert gas

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Pictograms

GHS07

Signal Word

Warning

Hazard Codes

H302,H317

Precautionary Statements

P261 - P264 - P272 - P280 - P301 + P312 - P302 + P352

Hazard Classifications

Acute Tox. 4 Oral - Skin Sens. 1A

Storage Class

11 - Combustible Solids

Flash Point (°F)

Not applicable

Flash Point (°C)