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.

• Sinonimo/i: γ-Secretase Inhibitor XXIV, BMS299897, 4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid, BMS-299897, BMS 299897
• Formula empirica (notazione di Hill): C₂₄H₂₁ClF₃NO₄S
• Numero CAS: 290315-45-6
• Peso molecolare: 511.94
• Numero MDL: MFCD12963627
• Codice UNSPSC: 12352200

Proprietà

• Livello qualitativo: 100
• Saggio: ≥97% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white
• Solubilità: ethanol: 100 mM; DMSO: 50 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: 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; IZAOBRWCUGOKNH-OAHLLOKOSA-N

Descrizione

Descrizione generale

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.

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.

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable