Avagacestat (BMS-708163)
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- Product name: Avagacestat (BMS-708163)
- CAS: 1146699-66-2
- MF: C20H17ClF4N4O4S
- MW: 520.89
- EINECS:
- MDL Number:MFCD13195458
- Synonyms:(2R)-2-[N-[(4-Chlorophenyl)sulfonyl]-N-[2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl]amino]-5,5,5-trifluoropentanamide;BMS-708163;(R)-2-(4-chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide;BMS-708163 (Avagacestat);Avagacestat;Avagacestat (BMS-708163);(R)-2-(4-Chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-phenylsulfonamido)-5,5,5-trifluoropen;(2R)-2-(N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-4-chlorophenylsulfonamido)-5,5,5-trifluoropentanamide
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Properties
Density :1.488
storage temp. :Store at -20°C
solubility :insoluble in H2O; ≥177.6 mg/mL in DMSO; ≥47.6 mg/mL in EtOH with ultrasonic
form :Powder
color :White to off-white
storage temp. :Store at -20°C
solubility :insoluble in H2O; ≥177.6 mg/mL in DMSO; ≥47.6 mg/mL in EtOH with ultrasonic
form :Powder
color :White to off-white
Safety Information
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Description
γ-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and β-amyloid precursor protein (APP), within the transmembrane domain. Avagacestat is a potent, orally bioavailable inhibitor of γ-secretase that more potently inhibits the cleavage of APP to Aβ40 than signaling through Notch (IC50s = 0.30 and 58 nM, respectively). It shows good pharmacokinetics in rats, dogs, and humans and passes the blood-brain barrier, reducing plasma, brain, and cerebrospinal fluid Aβ40 levels. While suppressing the production of Aβ38, Aβ40, and Aβ42, γ-secretase inhibitors, including avagacestat, increase the level of APP β-C-terminal fragment, both in vitro and in vivo, altering cell function. Avagacestat may impact Notch signaling in vivo, although it is generally considered a “Notch-sparing” γ-secretase inhibitor.More related product prices
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