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565793

γ-Secretase Inhibitor XXIV, BMS299897

Name: γ-Secretase Inhibitor XXIV, BMS299897
Brand: MM

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

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About This Item

Empirical Formula (Hill Notation):

C₂₄H₂₁ClF₃NO₄S

CAS Number:

290315-45-6

Molecular Weight:

511.94

UNSPSC Code:

12352200

MDL number:

MFCD12963627

Assay:

≥97% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

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Properties

Quality Level

100

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

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

InChI key

IZAOBRWCUGOKNH-OAHLLOKOSA-N

Description

General description

A cell-permeable sulfonamide compound that preferentially inhibits γ-secretase activity toward APP CTF over Notch-1 (IC₅₀ against APP_SW 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 APP_SW 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 APP_SW/APP_K670N/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

flash_point_f

Not applicable

flash_point_c