BMS 299897

SKU: orb1707537

Description

BMS 299897 is a potent sulfonamide γ-secretase inhibitor that effectively reduces Aβ peptide production, demonstrating an IC50 of 7 nM in APP-overexpressing HEK293 cells. This compound is a valuable research tool for investigating Alzheimer's disease pathogenesis in both cellular and animal models, targeting the amyloidogenic processing pathway.

Research Area

Neuroscience, Protein Biochemistry, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 290315-45-6
• MW: 511.94
• Purity: 99.82%
• Formula: C₂₄H₂₁ClF₃NO₄S
• SMILES: C[C@@H](N(c1cc(F)ccc1F)S(=O)(=O)c1ccc(Cl)cc1)c1ccc(F)cc1CCCC(O)=O
• Target: Gamma-secretase,Beta Amyloid
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.91 mM);DMSO:27 mg/mL (52.74 mM)

Bioactivity

• Target IC50:
  β-Amyloid (HEK293 cells):7 nM|β-Amyloid (HEK293 cells):7 nM
• In Vivo:
  BMS-299897 (0.1-1 nmol/mouse; male Swiss mice; one week) blocks the increase in Aβ1-42 content and decreases Aβ1-40 levels significantly. The compound does not affect the Aβ25-35-induced increase in hippocampal lipid peroxidation. Behaviorally, BMS-299897 blocks the Aβ25-35-induced deficits in spontaneous alternation or novel object recognition, using a 1 h intertrial time interval. The co-administration of the γ-secretase inhibitor BMS-299897, in the 0.1-1 μmol/mouse dose range, completely blocks the Aβ25-35-induced increase in Aβ1-42 content.
• In Vitro:
  BMS-299897 (1 μM) decreases these peptides to levels ranging from 20 to 50% of the vehicle control. Furthermore, it leads to a reduction in the proportion of QD-BDNF signals moving in the retrograde direction (p=0.0198) while concurrently increasing the proportion of signals moving in the anterograde direction (p=0.0147).

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Gammasecretase, BetaAmyloid, Beta Amyloid, BMS299897, BMS-299897, BMS 299897, Aβ, b Amyloid, bAmyloid, βAmyloid, β Amyloid, γ-secretase

Compound Identifiers

PubChem CID

11249248