Tiplaxtinin

SKU: orb1306703

Description

Tiplaxtinin (PAI-039) is a potent, selective, and orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), exhibiting an IC50 of 2.7 µM. It is a valuable research tool for studying fibrinolysis, thrombosis, and fibrosis in both cellular assays and animal models.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 393105-53-8
• MW: 439.38
• Purity: 99.93% (May vary between batches)
• Formula: C₂₄H₁₆F₃NO₄
• SMILES: OC(=O)C(=O)c1cn(Cc2ccccc2)c2ccc(cc12)-c1ccc(OC(F)(F)F)cc1
• Target: Apoptosis,PAI-1
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.55 mM);DMSO:50 mg/mL (113.8 mM);Ethanol:15 mg/mL (34.14 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PAI1:2.7 μM
• 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. In C57BL/6J mice, (1 mg/g chow) attenuates Ang II-induced aortic remodeling. In untreated type 1 diabetic mice, Tiplaxtinin (p.o.) restores skeletal muscle regeneration. 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.
• 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.
• Cell Research:
  Briefly, cell lines, T24, UM-UC-14, UROtsa, and HeLa cells are plated in 96-well dishes in triplicate at 1×103 cells per well and allowed to adhere for 24 hours. Subsequently, tiplaxtinin is added to the wells and allowed to incubate at the indicated concentrations. Cellular proliferation is determined by CellTiter-Glo Luminescent Cell Viability Assay according to manufacturer's instructions at 24 hours, and IC50 of tiplaxtinin is determined in Graphpad Prism. Luminescence was measured using a FLUOstar OPTIMA Reader.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Plasminogen activator inhibitor-1, Tiplasinin, Tiplaxtinin, Inhibitor, inhibit, PAI-1, PAI1, PAI039, PAI-039, PAI 039, Apoptosis

Compound Identifiers

PubChem CID

6450819