Diaplasinin (PAI-749) | PAI-1 inhibitor | Probechem Biochemicals

Chemical Structure : Diaplasinin

CAS No.: 481631-45-2

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Diaplasinin (PAI-749, PAI 749)

货号: 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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5 mg	￥1280	In stock
10 mg	￥1980	In stock
25 mg	￥3480	In stock
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	501.63
分子式	C32H31N5O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-benzyl-3-pentyl-2-[6-(1H-tetrazol-5-ylmethoxy)naphthalen-2-yl]-1H-indole

参考文献

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.

Diaplasinin (PAI-749, PAI 749)

生物&药学活性

物理化学性质&存储条件

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Diaplasinin (PAI-749, PAI 749)

生物&药学活性

物理化学性质&存储条件

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