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Chemical Structure : Diaplasinin
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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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.
| M.Wt | 501.63 | |
| Formula | C32H31N5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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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