Chemical Structure : Diaplasinin
CAS No.:
481631-45-2
Diaplasinin
(PAI-749, PAI 749)
Catalog No.: PC-49769Not For Human Use, Lab Use Only.
Diaplasinin (PAI-749) is a potent, selective antagonist of plasminogen activator inhibitor 1 (PAI-1) with IC50 of 154 nM (preservation of tPA activity) and Ki of 253 nM, blocks PAI-1 mediated inhibition of uPA with IC50 of 87 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Diaplasinin (PAI-749) is a potent, selective antagonist of plasminogen activator inhibitor 1 (PAI-1) with IC50 of 154 nM (preservation of tPA activity) and Ki of 253 nM, blocks PAI-1 mediated inhibition of uPA with IC50 of 87 nM.
Diaplasinin (PAI-749) dose-dependently blocked PAI-1-mediated inactivation of tPA activity toward its low-molecular-weight amidolytic substrate, Spectrozyme tPA.
Diaplasinin (PAI-749) displayed marked selectivity for PAI-1 relative to other serpins.
Diaplasinin (PAI-749) binds directly to PAI-1, blocks PAI-1 from accessing the active site of tPA, and abrogates formation of the SDS-stable tPA/PAI-1 complex.
PAI-749 does not affect thrombus formation or fibrinolysis in a range of established human plasma and whole blood-based systems.
Physicochemical Properties
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M.Wt
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501.63
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Formula
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C32H31N5O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-benzyl-3-pentyl-2-[6-(1H-tetrazol-5-ylmethoxy)naphthalen-2-yl]-1H-indole
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References
1. Gardell SJ, et al. Mol Pharmacol. 2007 Oct;72(4):897-906.
2. Lucking AJ, et al. J Thromb Haemost. 2010 Jun;8(6):1333-9.
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