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Tiplaxtinin(PAI-039)

(CAS No:393105-53-8)
Tiplaxtinin(PAI-039) is an orally efficacious and selective plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 2.7 μM.
CAS No:393105-53-8
Molecular Weight(MW):439.38
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 393105-53-8
Molecular formula(MF) C24H16F3NO4
Molecular Weight(MW): 439.38
Alias
Solubility
In vitro DMSO 72 mg/mL (163.86 mM)
Ethanol 18 mg/mL warmed (40.96 mM)
Water <1 mg/mL
In vivo 2.0% Tween 80+0.5% methylcellulose 30mg/mL
Biological Activity
Description Tiplaxtinin(PAI-039) is an orally efficacious and selective plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 2.7 μM.
Targets
PAI-1 [1]
2.7 μM
In vitro

In a panel of human bladder cell lines, PAI-1 results in the reduction of cellular proliferation, cell adhesion, and colony formation, and the induction of apoptosis and anoikis. [4]

In vivo In a rat carotid thrombosis model, Tiplaxtinin (1 mg/kg, p.o.) increases time to occlusion and prevents the carotid blood flow reduction. [1] In C57BL/6J mice, (1 mg/g chow) attenuates Ang II-induced aortic remodeling. [2] In untreated type 1 diabetic mice, Tiplaxtinin (p.o.) restores skeletal muscle regeneration. [3] In athymic mice bearing human cancer cell line T24 and HeLa xenografts, Tiplaxtinin (1 mg/kg, p.o.) reduces tumor xenograft growth, associated with a reduction in tumor angiogenesis, a reduction in cellular proliferation, and an increase in apoptosis. [4]