Details
Stereochemistry | ACHIRAL |
Molecular Formula | C29H27NO8 |
Molecular Weight | 517.5266 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)CCC1=C(OCC2=CC=C3C(=O)NOC3=C2)C=CC(=C1)C(=O)C4=C(O)C=C(OC5CCCC5)C=C4
InChI
InChIKey=DALCQQSLNPLQFZ-UHFFFAOYSA-N
InChI=1S/C29H27NO8/c31-24-15-21(37-20-3-1-2-4-20)8-10-22(24)28(34)19-6-11-25(18(14-19)7-12-27(32)33)36-16-17-5-9-23-26(13-17)38-30-29(23)35/h5-6,8-11,13-15,20,31H,1-4,7,12,16H2,(H,30,35)(H,32,33)
Molecular Formula | C29H27NO8 |
Molecular Weight | 517.5266 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2111421 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24831826 |
10.0 µM [IC50] |
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:18:26 GMT 2023
by
admin
on
Sat Dec 16 11:18:26 GMT 2023
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Record UNII |
3Z4EGU4HKZ
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Record Status |
Validated (UNII)
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Record Version |
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23626877
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R-7277
Created by
admin on Sat Dec 16 11:18:26 GMT 2023 , Edited by admin on Sat Dec 16 11:18:26 GMT 2023
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PRIMARY | Inhibitory activities: The DNA binding activity of transcription factors was measured using the TransAM kits (Active Motif). Nuclear extracts containing factors such as c-Fos/AP-1, c-Jun/AP-1, ATF-2, C/EBPa, MyoD, Sp-1 or NF-kB/p65 and various concentrations of T-5224 were added in the multi-well plates precoated with respective consensus double-stranded (ds)DNA oligomers. After incubation for 1 h, the transcription factor bound to its respective consensus dsDNA sequences was detected by using antibodies reactive against the respective transcription factors according to the manufacturers protocol. | ||
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530141-72-1
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DTXSID201026089
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3Z4EGU4HKZ
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admin on Sat Dec 16 11:18:26 GMT 2023 , Edited by admin on Sat Dec 16 11:18:26 GMT 2023
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ACTIVE MOIETY |
Treatment with T-5224 decreased serum TNF-.ALPHA. and HMGB-1 levels and increased survival after LPS injection. Furthermore, T-5224 treatment decreased serum BUN and creatinine concentrations but increased serum IL-10 concentration. LPS-induced pathological changes in kidney were attenuated by T-5224 treatment. These results suggest that T-5224, a selective inhibitor of c-Fos/AP-1, inhibits expression of early and late proinflammatory cytokines, protecting mice from LPS-induced lethality. T-5224 is a potential approach for decreasing lethality in sepsis-induced AKI.
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