Diaplasinin (Synonyms: PAI-749)
目录号: PL08752 纯度: ≥99%
CAS No. :481631-45-2
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中文名称
Diaplasinin
中文别名
1-苄基-3-戊基-2-(6-(1H-四唑-5-基甲氧基)萘-2-基)-1H-吲哚
英文名称
Diaplasinin
英文别名
1H-Indole,3-pentyl-1-(phenylmethyl)-2-[6-(2H-tetrazol-5-ylmethoxy)-2-naphthalenyl]-;1-benzyl-3-pentyl-2-[6-(2H-tetrazol-5-ylmethoxy)naphthalen-2-yl]indole;DIAPLASININ
Cas No.
481631-45-2
分子式
C32H31N5O
分子量
501.62
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Diaplasinin (PAI-749) 是纤溶酶原激活剂抑制剂-1 (PAI-1) 抑制剂,IC50 为 295 nm。具有抗血栓功效。
生物活性
Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC 50 of 295?nm. Antithrombotic efficacy.
性状
Solid
体外研究(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).
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 125 mg/mL (249.19 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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