481631-45-2

481631-45-2 structure

Name: Diaplasinin
Chemical Name: 1-benzyl-3-pentyl-2-[6-(2H-tetrazol-5-ylmethoxy)naphthalen-2-yl]indole
CAS Number: 481631-45-2
Molecular Formula: C₃₂H₃₁N₅O
Molecular Weight: 501.62100
Catalog: Signaling Pathways Metabolic Enzyme/Protease PAI-1
Create Date: 2017-04-05 19:09:02
Modify Date: 2024-01-31 17:33:09
Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nm. Antithrombotic efficacy[1].

Name	1-benzyl-3-pentyl-2-[6-(2H-tetrazol-5-ylmethoxy)naphthalen-2-yl]indole
Synonyms	PAI-749 UNII-NRL66AVH63 Diaplasinin

Description	Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nm. Antithrombotic efficacy[1].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> PAI-1 Research Areas >> Cardiovascular Disease
In Vitro	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].
References	[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.