For research use only. Not for therapeutic Use.
Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nM. Diaplasinin has antithrombotic efficacy[1].
PAI-749 is a potent and selective synthetic antagonist of plasminogen activator inhibitor 1 (PAI-1) that preserved tissue-type plasminogen activator (tPA) and urokinase-type plasminogen activator (uPA) activities in the presence of PAI-1 (IC50 values, 157 and 87 nM, respectively)[2].
PAI-749 quenches the fluorescence (Fl) of fluorophore-tagged PAI-1 (PAI-NBD119) with the apparent Kd of 254 nM) and the IC50 of 140 nM[2].
| Catalog Number | I012311 |
| CAS Number | 481631-45-2 |
| Synonyms | 1-benzyl-3-pentyl-2-[6-(2H-tetrazol-5-ylmethoxy)naphthalen-2-yl]indole |
| Molecular Formula | C32H31N5O |
| Purity | ≥95% |
| InChI | InChI=1S/C32H31N5O/c1-2-3-5-13-29-28-12-8-9-14-30(28)37(21-23-10-6-4-7-11-23)32(29)26-16-15-25-20-27(18-17-24(25)19-26)38-22-31-33-35-36-34-31/h4,6-12,14-20H,2-3,5,13,21-22H2,1H3,(H,33,34,35,36) |
| InChIKey | BDPXZFKVHDEPIQ-UHFFFAOYSA-N |
| SMILES | CCCCCC1=C(N(C2=CC=CC=C21)CC3=CC=CC=C3)C4=CC5=C(C=C4)C=C(C=C5)OCC6=NNN=N6 |
| Reference | [1]. A J Lucking, et al. Effect of the small molecule plasminogen activator inhibitor-1 (PAI-1) inhibitor, PAI-749, in clinical models of fibrinolysis. J Thromb Haemost. 2010 Jun;8(6):1333-9. [2]. Stephen J Gardell, et al. Neutralization of plasminogen activator inhibitor I (PAI-1) by the synthetic antagonist PAI-749 via a dual mechanism of action. Mol Pharmacol. 2007 Oct;72(4):897-906. |
