T-5224

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

T-5224 是 c-Fos/AP-1 的小分子抑制剂，特异性抑制 AP-1 与启动子区 AP-1 结合位点的结合，减弱 MMP-2 和 -9 的明胶酶活性。

T-5224 is a small molecule inhibitor of c-Fos/AP-1 that specifically inhibits the binding of AP-1 to the AP-1 binding site of the promoter region, attenuates the gelatinase activity of MMP-2 and -9; inhibits the mRNA expression levels of MMP-1, 3, and 13, and IL-1β, TNF-α and IL-6 in IL-1-stimulated human chondrocytes, significantly inhibits the invasion, migration, and MMP activity of HNSCC cells, prevents lymph node metastasis in an oral cancer model; decreases the release of collagen selectively in SSc fibroblasts, prevents dermal fibrosis in vivo.Rheumatoid Arthritis Phase 2 Discontinued(In Vitro):T-5224 inhibits in-vitro production of the mediators MMP-1, MMP-3, IL-6 and TNF-α by IL-1β-stimulated human synovial SW982 cells with the mean IC50 of about 10 μM.T-5224 (0-80 μM) significantly inhibits the invasion, migration, and MMP activity of HSC-3-M3 cells in a dose-dependent manner.(In Vivo):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%).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.T-5224 (300 mg/kg, p.o.) inhibits the production of TNF-alpha and other downstream effectors in C57BL/6 mice.

T-5224 inhibits in-vitro production of the mediators MMP-1, MMP-3, IL-6 and TNF-α by IL-1β-stimulated human synovial SW982 cells with the mean IC50 of about 10 μM.T-5224 (0-80 μM) significantly inhibits the invasion, migration, and MMP activity of HSC-3-M3 cells in a dose-dependent manner.

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%).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.T-5224 (300 mg/kg, p.o.) inhibits the production of TNF-alpha and other downstream effectors in C57BL/6 mice.

T5224 | T 5224

Nuclear Receptor/Transcription Factor

c-Fos/AP-1

c-Fos/AP-1

Inflammation/Immunology

Rheumatoid Arthritis

530141-72-1

517.5266

C29H27NO8

>98% (HPLC)

DMSO: ≥ 31 mg/mL

O=C(O)CCC1=CC(C(C2=CC=C(OC3CCCC3)C=C2O)=O)=CC=C1OCC4=CC5=C(C=C4)C(O)=NO5

Benzenepropanoic acid, 5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(2,3-dihydro-3-oxo-1,2-benzisoxazol-6-yl)methoxy]-

(-20℃)

With Ice Pack

≥ 2 years