Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C24H21ClF3NO4S |
| Molecular Weight | 511.941 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H](N(C1=CC(F)=CC=C1F)S(=O)(=O)C2=CC=C(Cl)C=C2)C3=C(CCCC(O)=O)C=C(F)C=C3
InChI
InChIKey=IZAOBRWCUGOKNH-OAHLLOKOSA-N
InChI=1S/C24H21ClF3NO4S/c1-15(21-11-7-18(26)13-16(21)3-2-4-24(30)31)29(23-14-19(27)8-12-22(23)28)34(32,33)20-9-5-17(25)6-10-20/h5-15H,2-4H2,1H3,(H,30,31)/t15-/m1/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/25710492 | https://www.ncbi.nlm.nih.gov/pubmed/15452193Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/15670587
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25710492 | https://www.ncbi.nlm.nih.gov/pubmed/15452193
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/15670587
BMS-299897 is an orally bioavailable, sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP). BMS-299897 has the potential for treatment of Alzheimer's disease.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15670587 | https://www.ncbi.nlm.nih.gov/pubmed/25291315
Curator's Comment: BMS-299897 markedly reduced both brain and plasma Abeta(1-40) in APP-YAC mice and in guinea pigs. Readily crosses blood–brain barrier.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Reductions in beta-amyloid concentrations in vivo by the gamma-secretase inhibitors BMS-289948 and BMS-299897. | 2005 Feb 15 |
|
| A γ-secretase inhibitor, but not a γ-secretase modulator, induced defects in BDNF axonal trafficking and signaling: evidence for a role for APP. | 2015 |
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11249248
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DTXSID50460039
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QK855F579S
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290315-45-6
Created by
admin on Sat Dec 16 16:34:18 GMT 2023 , Edited by admin on Sat Dec 16 16:34:18 GMT 2023
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ACTIVE MOIETY
