1. Metabolic Enzyme/Protease
  2. PAI-1 Ser/Thr Protease
  3. ZK824859

ZK824859 是一种口服有效的选择性尿激酶型纤溶酶原激活剂 (uPA) 抑制剂,用于人 uPA,tPA 和纤溶酶,IC50 分别为 79 nM,1580 nM 和 1330 nM。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 ZK824859 hydrochloride 通常具有更好的水溶性和稳定性。

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ZK824859 Chemical Structure

ZK824859 Chemical Structure

CAS No. : 2271122-53-1

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ZK824859 的其他形式现货产品:

Customer Review

Other Forms of ZK824859:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively[1].

IC50 & Target

IC50: 79 nM (human uPA), 1580 nM (human tPA), 1330 nM (human plasmin)[1].

体外研究
(In Vitro)

ZK824859 is 5 fold less potent and has lost selectivity in mouse: uPA IC50=410 nM; tPA IC50=910 nM; plasmin IC50=1600 nM compared to human IC50 values of 79 nM, 1580 nM and 1330 nM respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

ZK824859 (50, 25 and 10 mg/kg; b.i.d.; 25 days) is used in a chronic mouse EAE model. ZK 824859 completely prevents the development of disease. However, two lower doses (25 and 10 mg/kg) have no effect on clinical scores[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female SJL mice with chronic mouse EAE model[1]
Dosage: 50, 25 and 10 mg/kg
Administration: B.i.d.; 25 days
Result: Prevented the development of disease at 50 mg/kg completely. However, 25 and 10 mg/kg had no effect on clinical scores.
分子量

428.43

Formula

C23H22F2N2O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ZK824859
目录号:
HY-114330
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