For research use only. Not for therapeutic Use.
Tiplaxtinin（Cat No.:I003439）, also known as PAI-039, is a selective inhibitor of plasminogen activator inhibitor-1 (PAI-1), a protein involved in blood clot regulation and fibrosis. By blocking PAI-1 activity, Tiplaxtinin enhances fibrinolysis, promoting the breakdown of blood clots, and is studied for its potential therapeutic benefits in thrombotic and cardiovascular diseases. It has also shown promise in research on fibrosis and certain metabolic disorders where PAI-1 is implicated. Tiplaxtinin’s targeted mechanism makes it valuable for exploring treatment avenues in cardiovascular health, fibrosis, and related inflammatory conditions.
| Catalog Number | I003439 |
| CAS Number | 393105-53-8 |
| Synonyms | PAI-039;Tiplasinin |
| Molecular Formula | C₂₄H₁₆F₃NO₄ |
| Purity | ≥95% |
| Target | PAI-1 inhibitor |
| Solubility | DMSO: ≥ 54 mg/mL |
| Storage | -20°C |
| IC50 | 2.7 uM |
| IUPAC Name | 2-[1-benzyl-5-[4-(trifluoromethoxy)phenyl]indol-3-yl]-2-oxoacetic acid |
| InChI | InChI=1S/C24H16F3NO4/c25-24(26,27)32-18-9-6-16(7-10-18)17-8-11-21-19(12-17)20(22(29)23(30)31)14-28(21)13-15-4-2-1-3-5-15/h1-12,14H,13H2,(H,30,31) |
| InChIKey | ODXQFEWQSHNQNI-UHFFFAOYSA-N |
| SMILES | C1=CC=C(C=C1)CN2C=C(C3=C2C=CC(=C3)C4=CC=C(C=C4)OC(F)(F)F)C(=O)C(=O)O |
| Reference | </br>1:Effect of tiplaxtinin (PAI-039), an orally bioavailable PAI-1 antagonist, in a rat model of thrombosis. Hennan JK, Morgan GA, Swillo RE, Antrilli TM, Mugford C, Vlasuk GP, Gardell SJ, Crandall DL.J Thromb Haemost. 2008 Sep;6(9):1558-64. doi: 10.1111/j.1538-7836.2008.03063.x. Epub 2008 Jul 4. PMID: 18624980 Free Article</br>2:Dose-dependent thrombus resolution due to oral plaminogen activator inhibitor (PAI)-1 inhibition with tiplaxtinin in a rat stenosis model of venous thrombosis. Baxi S, Crandall DL, Meier TR, Wrobleski S, Hawley A, Farris D, Elokdah H, Sigler R, Schaub RG, Wakefield T, Myers D.Thromb Haemost. 2008 Apr;99(4):749-58. doi: 10.1160/TH07-11-0669. PMID: 18392333 </br>3:Tiplaxtinin impairs nutritionally induced obesity in mice. Lijnen HR, Alessi MC, Frederix L, Collen D, Juhan-Vague I.Thromb Haemost. 2006 Dec;96(6):731-7. PMID: 17139366 </br>4:Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization. Elokdah H, Abou-Gharbia M, Hennan JK, McFarlane G, Mugford CP, Krishnamurthy G, Crandall DL.J Med Chem. 2004 Jul 1;47(14):3491-4. PMID: 15214776 |
