Cas No.: | 530141-72-1 |
Chemical Name: | 3-(5-(4-(cyclopentyloxy)-2-hydroxybenzoyl)-2-((3-hydroxybenzo[d]isoxazol-6-yl)methoxy)phenyl)propanoic acid |
Synonyms: | T-5224; T5224; T 5224. |
SMILES: | C(CCC(O)=O)1=CC(C(=O)C2=CC=C(OC3CCCC3)C=C2O)=CC=C1OCC1=CC2=C(C=C1)C(=O)NO2 |
Formula: | C29H27NO8 |
M.Wt: | 517.53 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | T-5224 is a selective inhibitor of c-Fos/activator protein (AP)-1. It also inhibits MMP3/13 with IC50s of 10 nM. |
In Vivo: | G2 is observed in rat and monkey liver microsomes as a major metabolite of T-5224, suggesting that G2 is not a human-specific metabolite[1]. T-5224 (300 mg/kg, p.o.) inhibits the production of TNF-alpha and other downstream effectors in C57BL/6 mice[2]. Administration of T-5224 (300 mg/kg, p.o.) after intraperitoneal injection of LPS impartes appreciable protection against acute elevations in serum levels of TNFα, HMGB1, ALT/AST as well as in liver tissue levels of MIP-1α and MCP-1, and reduces the lethality (27%)[3]. |
In Vitro: | T-5224 (0-80 μM) significantly inhibits the invasion, migration, and MMP activity of HSC-3-M3 cells in a dose-dependent manner. There is no significant influence on HSC-3-M3 amd OSC-19 cells proliferation[4]. |