Skip to Content
Merck

565793

γ-Secretase Inhibitor XXIV, BMS299897

The γ-Secretase Inhibitor XXIV, BMS299897, also referenced under CAS 290315-45-6, controls the biological activity of γ-Secretase. This small molecule/inhibitor is primarily used for Neuroscience applications.

Synonym(s):

γ-Secretase Inhibitor XXIV, BMS299897, 4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid, BMS-299897, BMS 299897

Sign In to View Organizational & Contract Pricing.

Select a Size


About This Item

Empirical Formula (Hill Notation):
C24H21ClF3NO4S
CAS Number:
Molecular Weight:
511.94
UNSPSC Code:
12352200
MDL number:
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist

InChI key

IZAOBRWCUGOKNH-OAHLLOKOSA-N

InChI

1S/C24H21ClF3NO4S/c1-15(21-11-7-18(26)13-16(21)3-2-4-24(30)31)29(23-14-19(27)8-12-22(23)28)34(32,33)20-9-5-17(25)6-10-20/h5-15H,2-4H2,1H3,(H,30,31)/t15-/m1/s1

SMILES string

FC1=CC(CCCC(O)=O)=C([C@@H](C)N(S(=O)(C2=CC=C(Cl)C=C2)=O)C3=C(F)C=CC(F)=C3)C=C1

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

ethanol: 100 mM, DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

General description

A cell-permeable sulfonamide compound that preferentially inhibits γ-secretase activity toward APP CTF over Notch-1 (IC50 against APPSW CTF and murine ΔE-Notch processing = 7.1 and 105.9 nM, respectively, in HEK293) in a presenillin 1-/PS1-selective manner (IC50 = 8 and 308 nM against APPSW processing in PS1-/-PS2-/-MEF expressing human PS1 and PS2, respectively). BMS-299897 is shown to be orally available, readily cross blood-brain-barrier (<15 min), and effectively suppress plasma and brain Aβ level in transgenic mice bearing normal human APP (APP-YAC) or APPSW/APPK670N/M671L (Tg2576) in a time- and dose-dependent manner (optimal p.o. dose 100 mg/kg) in vivo. However, BMS-299897 is not effective in reducing Aβ in aged, plaque-bearing murine brain and long-term daily drug dosing is reported to result in increased drug metabolizing activity in mice.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Zhao, B., et al. 2008. J. Biol. Chem. 283, 2927.
Barten, D.M., et al. 2005. J. Pharmacol. Exp. Ther.312, 635.
Anderson, J.J., et al. 2005. Biochem. Pharmacol.69, 689.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service