Millipore Sigma Vibrant Logo
Attention: We have moved. EMD Millipore products are no longer available for purchase on emdmillipore.com.Learn More

565793 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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: BMS-299897, BMS 299897, 4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid

View Products on Sigmaaldrich.com
565793
  
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
290315-45-6C₂₄H₂₁ClF₃NO₄S
Description
OverviewA 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.
Catalogue Number565793
Brand Family Calbiochem®
SynonymsBMS-299897, BMS 299897, 4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid
References
ReferencesZhao, 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.
Product Information
CAS number290315-45-6
FormWhite solid
Hill FormulaC₂₄H₂₁ClF₃NO₄S
Chemical formulaC₂₄H₂₁ClF₃NO₄S
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

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

Title

Safety Data Sheet (SDS) 

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

TitleLot Number
565793

References

Reference overview
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.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision16-April-2012 JSW
SynonymsBMS-299897, BMS 299897, 4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid
DescriptionA 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.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number290315-45-6
Chemical formulaC₂₄H₂₁ClF₃NO₄S
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (50 mg/ml) Ethanol (100 mM)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesZhao, 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.