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BM0005 Sigma-Aldrich

Avagacestat

≥98% (HPLC)

Synonym: (2R)-2-[N-[(4-Chlorophenyl)sulfonyl]-N-[[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide, (R)-2-(4-Chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide, BMS-708163

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Properties

Related Categories AN-AZ, Alzheimer′s Disease, Assays/Reagents for Alzheimer′s Disease Research, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules,
Quality Level   100
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 30 mg/mL, clear
storage temp.   room temp
SMILES string   NC([C@@H](CCC(F)(F)F)N(S(C1=CC=C(Cl)C=C1)(=O)=O)CC2=C(F)C=C(C3=NOC=N3)C=C2)=O
InChI   1S/C20H17ClF4N4O4S/c21-14-3-5-15(6-4-14)34(31,32)29(17(18(26)30)7-8-20(23,24)25)10-13-2-1-12(9-16(13)22)19-27-11-33-28-19/h1-6,9,11,17H,7-8,10H2,(H2,26,30)/t17-/m1/s1
InChI key   XEAOPVUAMONVLA-QGZVFWFLSA-N
Gene Information   human ... APH1A(51107), APH1B(83464), NCSTN(23385), PSEN1(5663), PSEN2(5664), PSENEN(55851)

Description

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

Avagacestat (BMS-708163) is a potent γ-secretase inhibitor selective for amyloid precursor protein (APP) over Notch cleavage. Avagacestat inhibits Aβ40 and Aβ42 production with IC50 values of 0.3 nM and 0.27 nM, respectively, compared to IC50 values of 41, 10, 33, and 38 nM respectively for signaling inhibition of the human Notch 1-4 proteins. At higher concentrations BMS-708163 has been found to reverse sensitivity to the EGFR tyrosine kinase inhibitor gefitinib, thought to be by Notch inhibition.

Features and Benefits

Avagacestat is available through a partnership with Bristol-Myers Squibb (BMS). To learn more and view other BMS compounds, visit sigma.com/BMS.

Legal Information

Sold for research purposes only under agreement from BMS.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis (COA)

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Protocols & Articles

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