Avagacestat

Name: Avagacestat
Brand: Tocris Bioscience
SKU: 6363

Tocris Bioscience, part of Bio-Techne | Catalog # 6363

Citations (1)

COA / SDS

Highly potent γ-secretase inhibitor; orally bioavailable

Key Product Details

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)
Molecular Weight:	520.89

View Full Technical Details for Avagacestat

Technical Data
Citations

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
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 for Avagacestat

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.92 mL	9.60 mL	19.20 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.

Albright Pharmacodynamics of selective inhibition of γ-secretase by avagacestat. J.Pharmacol.Exp.Ther. 2013 PMID: 23275065
Gillman Discovery and evaluation of BMS-708163, a potent, selective and orally bioavailable γ-secretase inhibitor. ACS Med.Chem.Lett. 2010 PMID: 24900185