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565793

Sigma-Aldrich

γ-Secretase Inhibitor XXIV, BMS299897 - CAS 290315-45-6 - Calbiochem

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 - CAS 290315-45-6 - Calbiochem, 4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid, BMS-299897, BMS 299897
Empirical Formula (Hill Notation):
C24H21ClF3NO4S
CAS Number:
Molecular Weight:
511.94
MDL number:

Quality Level

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

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

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.
A cell-permeable sulfonamide compound that preferentially inhibits cellular γ-secretase cleavage of APP CTF over Notch-1 (IC50 = 7.1 and 105.9 nM, respectively) in a presenillin 1-/PS1-selective manner (IC50 = 8 and 308 nM against 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 human APP-bearing transgenic mice in a time- and dose-dependent manner (optimal p.o. dose 100 mg/kg) in vivo.

Packaging

5 mg in Glass bottle
Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis

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Certificate of Quality

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