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Tiplaxtinin

Tiplaxtinin inhibits plasminogen activator inhibitor 1 (PAI-1), decreasing would closure and collagen deposition. Tiplaxtinin exhibits anti-inflammatory, anti-fibrotic, anti-allergic, anti-angiogenic, and anticancer chemotherapeutic activities. Tiplaxtinin inhibits carotid artery neointimal formation and increases apoptosis in vascular smooth muscle cells. In models of bladder cancer, this compound inhibits angiogenesis, increases apoptosis, and decreases cell proliferation, cell adhesion, and tumor growth. Tixplatinin also decreases inflammation, collagen deposition, and airway hyperresponsiveness in animal models of OVA-induced pulmonary remodeling.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18976560

Cas No.

393105-53-8

Formula

C24H16F3NO4

Formula Wt.

439.39

IUPAC Name

{1-Benzyl-5-[4-(trifluoromethoxy)phenyl]-1H-indol-3-yl}(oxo)acetic acid

Synonym

PAI-039

Simone TM, Longmate WM, Law BK, et al. Targeted Inhibition of PAI-1 Activity Impairs Epithelial Migration and Wound Closure Following Cutaneous Injury. Adv Wound Care (New Rochelle). 2015 Jun 1;4(6):321-328. PMID: 26029482.

Simone TM, Higgins SP, Archambeault J, et al. A small molecule PAI-1 functional inhibitor attenuates neointimal hyperplasia and vascular smooth muscle cell survival by promoting PAI-1 cleavage. Cell Signal. 2015 May;27(5):923-33. PMID: 25617690.

Gomes-Giacoia E, Miyake M, Goodison S, et al. Targeting plasminogen activator inhibitor-1 inhibits angiogenesis and tumor growth in a human cancer xenograft model. Mol Cancer Ther. 2013 Dec;12(12):2697-708. PMID: 24072883.

Lee SH, Eren M, Vaughan DE, et al. A plasminogen activator inhibitor-1 inhibitor reduces airway remodeling in a murine model of chronic asthma. Am J Respir Cell Mol Biol. 2012 Jun;46(6):842-6. PMID: 22323366.

ABT 628