Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- T-5224
- DrugBank Accession Number
- DB05998
- Background
T-5224 is an investigational drug developed to treat Sepsis-induced Acute Kidney Injury. It's mechanism of action is to inhibit c-Fos/activator protein-1.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for T-5224 (DB05998)
- Weight
- Average: 517.534
Monoisotopic: 517.173666833 - Chemical Formula
- C29H27NO8
- Synonyms
- Not Available
- External IDs
- 3-(5-(4-(CYCLOPENTOXY)-2-HYDROXY-BENZOYL)-2-((3-HYDROXY-1,2-BENZOXAZOL-6-YL)METHOXY)PHENYL)PROPANOIC ACID
- BENZENEPROPANOIC ACID, 5-(4-(CYCLOPENTYLOXY)-2-HYDROXYBENZOYL)-2-((2,3-DIHYDRO-3-OXO-1,2-BENZISOXAZOL-6-YL)METHOXY)-
- R-7277
- T5224
Pharmacology
- Indication
Investigated for use/treatment in rheumatoid arthritis.
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Not Available
- Mechanism of action
T-5224 is an inhibitor of the transcription factor AP-1 (Activator Protein-1) which is known to play an important role in the pathology of rheumatoid arthritis. AP-1 turns on a variety of genes in response to inflammation triggers, including many that are responsible for the proteins that are the targets of current rheumatoid arthritis products. In addition, in joint cells called osteoclasts, AP-1 stimulates the production of enzymes that are thought specifically to cause the destruction of bones and joint tissue. Therefore, by inhibiting the AP-1 process, T-5224 affects several key pathways and may prevent the progression of this disabling disease in many patients.
Target Actions Organism ATranscription factor Jun inhibitorHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- Not Available
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 3Z4EGU4HKZ
- CAS number
- 530141-72-1
- InChI Key
- DALCQQSLNPLQFZ-UHFFFAOYSA-N
- InChI
- 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)
- IUPAC Name
- SMILES
- OC(=O)CCC1=CC(=CC=C1OCC1=CC2=C(C=C1)C(O)=NO2)C(=O)C1=C(O)C=C(OC2CCCC2)C=C1
References
- General References
- Ishida M, Ueki M, Morishita J, Ueno M, Shiozawa S, Maekawa N: T-5224, a selective inhibitor of c-Fos/activator protein-1, improves survival by inhibiting serum high mobility group box-1 in lethal lipopolysaccharide-induced acute kidney injury model. J Intensive Care. 2015 Nov 14;3:49. doi: 10.1186/s40560-015-0115-2. eCollection 2015. [Article]
- External Links
- Human Metabolome Database
- HMDB0258662
- ChemSpider
- 25069717
- BindingDB
- 50044561
- ChEMBL
- CHEMBL3222137
- ZINC
- ZINC000003816510
Clinical Trials
- Clinical Trials
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Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Transcription factor that recognizes and binds to the AP-1 consensus motif 5'-TGA[GC]TCA-3' (PubMed:10995748, PubMed:22083952). Heterodimerizes with proteins of the FOS family to form an AP-1 transcription complex, thereby enhancing its DNA binding activity to the AP-1 consensus sequence 5'-TGA[GC]TCA-3' and enhancing its transcriptional activity (By similarity). Together with FOSB, plays a role in activation-induced cell death of T cells by binding to the AP-1 promoter site of FASLG/CD95L, and inducing its transcription in response to activation of the TCR/CD3 signaling pathway (PubMed:12618758). Promotes activity of NR5A1 when phosphorylated by HIPK3 leading to increased steroidogenic gene expression upon cAMP signaling pathway stimulation (PubMed:17210646). Involved in activated KRAS-mediated transcriptional activation of USP28 in colorectal cancer (CRC) cells (PubMed:24623306). Binds to the USP28 promoter in colorectal cancer (CRC) cells (PubMed:24623306)
- Specific Function
- Camp response element binding
- Gene Name
- JUN
- Uniprot ID
- P05412
- Uniprot Name
- Transcription factor Jun
- Molecular Weight
- 35675.32 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
Drug created at November 18, 2007 18:29 / Updated at August 26, 2024 19:22