2. Metabolic Enzyme/Protease
  3. Elastase
  4. Freselestat quarterhydrate

Freselestat quarterhydrate  (Synonyms: ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate)

目录号: HY-15652A 纯度: ≥99.0%
COA 产品使用指南

摩尔计算器

Freselestat quarterhydrate (ONO-6818 quarterhydrate) 是一种有效且具有口服活性的嗜中性粒细胞弹性蛋白酶 (neutrophil elastase) 抑制剂，Ki 为 12.2 nM。Freselestat quarterhydrate 对其他蛋白酶（例如胰蛋白酶，蛋白酶3，胰弹性蛋白酶，纤溶酶，凝血酶，胶原酶，组织蛋白酶G和鼠巨噬细胞弹性蛋白酶）的活性低 100 倍以上，并具有有效的抗炎活性。

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Freselestat quarterhydrate Chemical Structure

Freselestat quarterhydrate Chemical Structure

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规格 价格 是否有货 数量
1 mg ￥2136
In-stock
5 mg ￥4700
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Customer Review

Other Forms of Freselestat quarterhydrate:

Freselestat quarterhydrate 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity[1][2][3][4].

IC50 & Target

Ki: 12.2 nM (Neutrophil elastase)[3]
体外研究
(In Vitro)

Simulated extracorporeal circulation is established by recirculating fresh heparinized (3.75 U/mL) human blood for 120 minutes in a membrane oxygenator and a roller pump with and without 1.0 μM of Freselestat (ONO-6818). Neutrophil elastase levels are significantly lower in the Freselestat group. Freselestat significantly reduces interleukin 8 and C5b-9 production. Freselestat does not modulate changes of CD11b and L-selectin during recirculation[3].

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

Freselestat quarterhydrate 相关抗体:
体内研究
(In Vivo)

Freselestat (ONO-6818; 10-100 mg/kg; oral administration; daily; for 8 weeks) treatment attenuates dose-dependently HNE-induced increases in lung myeloperoxidase activity, hemoglobin, and neutrophil count in bronchoalveolar lavage fluid. ONO-6818 inhibits acute lung injury induced by HNE by minimizing lung hemorrhage and accumulation of neutrophils in the lung[1].

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

Animal Model: Male Wistar rats (228 g) induced by human neutrophil elastase (HNE)[1]
Dosage: 10 mg/kg, 100 mg/kg
Administration: Oral administration; daily; for 8 weeks
Result: Attenuated dose-dependently HNE-induced increases in lung myeloperoxidase activity, hemoglobin, and neutrophil count in bronchoalveolar lavage fluid.
分子量

457.03

Formula

C23H28N6O4.1/4H2O
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 40 mg/mL (87.52 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1880 mL 10.9402 mL 21.8804 mL
5 mM 0.4376 mL 2.1880 mL 4.3761 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥99.0%

COA (198 KB) 元素分析报告 (214 KB)

产品使用指南 (1538 KB)
参考文献

Freselestat quarterhydrate 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1880 mL 10.9402 mL 21.8804 mL 54.7010 mL
5 mM 0.4376 mL 2.1880 mL 4.3761 mL 10.9402 mL
10 mM 0.2188 mL 1.0940 mL 2.1880 mL 5.4701 mL
15 mM 0.1459 mL 0.7293 mL 1.4587 mL 3.6467 mL
20 mM 0.1094 mL 0.5470 mL 1.0940 mL 2.7351 mL
25 mM 0.0875 mL 0.4376 mL 0.8752 mL 2.1880 mL
30 mM 0.0729 mL 0.3647 mL 0.7293 mL 1.8234 mL
40 mM 0.0547 mL 0.2735 mL 0.5470 mL 1.3675 mL
50 mM 0.0438 mL 0.2188 mL 0.4376 mL 1.0940 mL
60 mM 0.0365 mL 0.1823 mL 0.3647 mL 0.9117 mL
80 mM 0.0274 mL 0.1368 mL 0.2735 mL 0.6838 mL
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.

Keywords:

Freselestat quarterhydrateONO-6818 quarterhydrateONO-PO-736 quarterhydrateElastaseNon-peptidicorallyneutrophilelastaseIL-8C5b-9myeloperoxidaseanti-inflammatoryInhibitorinhibitorinhibit

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目录号：
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