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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)
Citations (1)
Literature (2)

Biological Activity for Avagacestat

Avagacestat is a 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.

Compound Libraries for Avagacestat

Avagacestat is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Avagacestat

M. Wt 520.89
Formula C20H17ClF4N4O4S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1146699-66-2
PubChem ID 46883536
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 for Avagacestat

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

Preparing Stock Solutions for Avagacestat

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

Select a batch to recalculate based on the batch molecular weight:
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 for Avagacestat

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

If you know of a relevant reference for Avagacestat, please let us know.

View Related Products by Product Action

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

1 Citation for Avagacestat

Citations are publications that use Tocris products. Selected citations for Avagacestat include:

Wulf et al (2021) Roles for ADAM17 in TNF-R1 Mediated Cell Death and Survival in Human U937 and Jurkat Cells. Cells 10 PMID: 34831323

Do you know of a great paper that uses Avagacestat from Tocris? Please let us know.

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