Metabolism PAI-1 Tiplaxtinin


Catalog No. T2030   CAS 393105-53-8
Synonyms: Tiplasinin, PAI-039

Tiplaxtinin(PAI-039) is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 uM.

Tiplaxtinin, CAS 393105-53-8
Pack Size Availability Price/USD Quantity
2 mg In stock 50.00
5 mg In stock 77.00
10 mg In stock 97.00
25 mg In stock 174.00
100 mg In stock 637.00
1 mL * 10 mM (in DMSO) In stock 81.00
Bulk Inquiry
Select Batch  
Purity 99.26%
Purity 99.49%
Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Tiplaxtinin(PAI-039) is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 uM.
Targets&IC50 PAI-1 : ic50 2.7μM
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]
Kinase Assay Direct PAI-I in vitro activity assays : The chromogenic assay is initiated by the addition of tiplaxtinin (10 – 100 µM final concentration, maximum DMSO concentration of 0.2%) to recombinant human PAI-1 (140 nM in pH 6.6 buffer). After a 15 minute incubation at 25°C, 70 nM of recombinant human t-PA is added, and the combination of tiplaxtinin, PAI-1 and tPA are incubated for an additional 30 minutes. After the second incubation, Spectrozyme tPA, is added and absorbance read at 405 nm at 0 and 60 minutes. Relative PAI-1 inhibitory activity is equal to the residual tPA activity in the tiplaxtinin / PAI-1 treatment. Control treatments include the complete inhibition of tPA by PAI-1 at the molar ratio employed (2:1), and the absence of any effect of the tiplaxtinin on t-PA alone. The immunofunctional assay is based upon the non-SDS dissociable interaction between tPA and active PAI-1. Assay plates are coated with 100 µl of a solution of t-PA (10 µg/ml in TBS), and kept at 4 °C overnight. Tiplaxtinin is dissolved in DMSO and diluted to a final concentration of 1-100 µM as described above. Tiplaxtinin is then incubated with human PAI-1 (50 ng/ml) for 15 minutes, and an aliquot of this solution added to the t-PA-coated plate for 1 h. The solution is aspirated from the plate, which is then washed with a buffer consisting of 0.05% Tween 20 and 0.1% BSA in TBS. This assay detects only active inhibitory PAI-1 (not latent or substrate) bound to the plate, and is quantitated using a monoclonal antibody against human PAI-1 (MA33B8). A 1000X dilution of MA33B8 is added to the plate and incubated at for one hour, aspirated and washed. A secondary antibody consisting of goat anti-mouse IgG (H+L)-AP alkaline phosphatase conjugate is added, incubated for one hour, aspirated and washed. A 100 µl aliquot of alkaline phosphatase solution is added, followed by determination of absorbance at 405 nm 60 minutes later. The quantitation of residual active PAI-1 bound to t-PA at varying concentrations of tiplaxtinin is used to determine the IC50 by fitting the results to a logistic dose-response program, with the IC50 defined as the concentration of compound required to achieve 50% inhibition of PAI-1 activity. The assay sensitivity is 5 ng/ml of human PAI-1 as determined from a standard curve ranging from 0-100 ng/ml of human PAI-1.
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)
Cell lines: T24, UM-UC-14, UROtsa, and HeLa cells
Animal Research
Animal Model: Rat with carotid thrombosis
Synonyms Tiplasinin , PAI-039
Purity 99.26%
Molecular Weight 439.38
Formula C24H16F3NO4
CAS No. 393105-53-8


0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 67 mg/mL (152.5 mM)

Ethanol: 15 mg/mL (34.1 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )


References and Literature
1. Elokdah H, et al. J Med Chem. 2004, 47(14), 3491-3494. 2. Weisberg AD, et al. Arterioscler Thromb Vasc Biol. 2005, 25(2), 365-371. 3. Krause MP, et al. Diabetes. 2011, 60(7), 1964-1972. 4. Gomes-Giacoia E, et al. Mol Cancer Ther. 2013, 12(12), 2697-2708.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Clinical Compound Library Apoptosis Compound Library Autophagy Compound Library Protease Inhibitor Library Bioactive Lipid Compound Library Fluorochemical Library Anti-Metabolism Disease Compound Library Anti-Cardiovascular Disease Compound Library

Related Products

Related compounds with same targets
Tiplaxtinin Loureirin B Calceolarioside B TM5441 TM5275 sodium Toddalolactone TM5007

Dose Conversion

Safe and effective drug dosing is necessary, regardless of its purpose of administration. Learn More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Average weight of animals
Dosing volume per animal
Number of animals
Step Two: Enter the in vivo formulation
% Tween 80
% ddH2O
Calculate Reset


Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator

Molarity Calculator allows you to calculate the

  • mass of a compound required to prepare a solution of known volume and concentration
  • volume of solution required to dissolve a compound of known mass to a desired concentration
  • concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box


Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box


Calculate the volume of solvent required to reconstitute your vial

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.


Tech Support

Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.