Avagacestat

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Cat.No. 6363 - Avagacestat | C20H17ClF4N4O4S | CAS No. 1146699-66-2
Description: Highly potent γ-secretase inhibitor; orally bioavailable
Alternative Names: BMS-708163
Chemical Name: (2R)-2-[[(4-Chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Highly potent γ-secretase inhibitor (Aβ40 IC50 = 0.3 nM). Exhibits >137-fold selectivity for amyloid-β precursor protein (APP) processing over Notch. Reduces plasma and brain Aβ40 and Aβ42 levels in vivo. Orally bioavailable.

Technical Data

M. Wt 520.89
Formula C20H17ClF4N4O4S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1146699-66-2
PubChem ID 46883536
InChI Key XEAOPVUAMONVLA-QGZVFWFLSA-N
Smiles NC([C@H](N(S(=O)(C1=CC=C(C=C1)Cl)=O)CC2=C(C=C(C3=NOC=N3)C=C2)F)CCC(F)(F)F)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 52.09 100
ethanol 10.42 20

Preparing Stock Solutions

The following data is based on the product molecular weight 520.89. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.92 mL 9.6 mL 19.2 mL
5 mM 0.38 mL 1.92 mL 3.84 mL
10 mM 0.19 mL 0.96 mL 1.92 mL
50 mM 0.04 mL 0.19 mL 0.38 mL

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References

References are publications that support the biological activity of the product.

Gillman et al (2010) Discovery and evaluation of BMS-708163, a potent, selective and orally bioavailable γ-secretase inhibitor. ACS Med.Chem.Lett. 1 120 PMID: 24900185

Albright et al (2013) Pharmacodynamics of selective inhibition of γ-secretase by avagacestat. J.Pharmacol.Exp.Ther. 344 686 PMID: 23275065


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View all γ-Secretase Inhibitors

Keywords: Avagacestat, Avagacestat supplier, gamma, γ, secretase, inhibitors, inhibits, Abeta, AB, Aβ40, 42, amyloid-β, precursor, protein, APP, processing, highly, potent, BMS-708163, Gamma-Secretase, Amyloid, Beta, Peptides, 6363, Tocris Bioscience

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