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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
Structure of R-7277

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)

HIDE SMILES / InChI

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

Targets

Primary TargetPharmacologyConditionPotency
10.0 µM [IC50]
Substance Class Chemical
Created
by admin
on Sat Dec 16 11:18:26 GMT 2023
Edited
by admin
on Sat Dec 16 11:18:26 GMT 2023
Record UNII
3Z4EGU4HKZ
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
R-7277
Common Name English
BENZENEPROPANOIC ACID, 5-(4-(CYCLOPENTYLOXY)-2-HYDROXYBENZOYL)-2-((2,3-DIHYDRO-3-OXO-1,2-BENZISOXAZOL-6-YL)METHOXY)-
Systematic Name English
3-(5-(4-(CYCLOPENTOXY)-2-HYDROXY-BENZOYL)-2-((3-HYDROXY-1,2-BENZOXAZOL-6-YL)METHOXY)PHENYL)PROPANOIC ACID
Systematic Name English
T5224
Code English
T-5224
Code English
5-(4-(CYCLOPENTYLOXY)-2-HYDROXYBENZOYL)-2-((2,3-DIHYDRO-3-OXO-1,2-BENZISOXAZOL-6-YL)METHOXY)BENZENEPROPANOIC ACID
Systematic Name English
Code System Code Type Description
PUBCHEM
23626877
Created by admin on Sat Dec 16 11:18:26 GMT 2023 , Edited by admin on Sat Dec 16 11:18:26 GMT 2023
PRIMARY
MANUFACTURER PRODUCT INFORMATION
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
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.
CAS
530141-72-1
Created by admin on Sat Dec 16 11:18:26 GMT 2023 , Edited by admin on Sat Dec 16 11:18:26 GMT 2023
PRIMARY
EPA CompTox
DTXSID201026089
Created by admin on Sat Dec 16 11:18:26 GMT 2023 , Edited by admin on Sat Dec 16 11:18:26 GMT 2023
PRIMARY
FDA UNII
3Z4EGU4HKZ
Created by admin on Sat Dec 16 11:18:26 GMT 2023 , Edited by admin on Sat Dec 16 11:18:26 GMT 2023
PRIMARY
Related Record Type Details
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.