Sivelestat sodium tetrahydrate (Synonyms:西维来司钠四水合物; EI546 sodium tetrahydrate; LY544349 sodium tetrahydrate; ONO5046 sodium tetrahydrate)
目录号 : KM16861 CAS No. : 201677-61-4 纯度 : 98%

Sivelestat (EI546) sodium tetrahydrate 是竞争性的人类中性粒细胞弹性蛋白酶的抑制剂,其 IC50 值为 44 nM, Ki 值为 200 nM。Sivelestat (EI546) sodium tetrahydrate 有潜力用于COVID-19的急性肺损伤/急性呼吸窘迫综合征或弥散性血管内凝血的研究。

规格 价格 是否有货 数量
10mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.

体外研究

Sivelestat (ONO-5046) does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM.
Sivelestat (ONO-5046) exhibits IC50 values of 44 nM, 36 nM, 19 nM, 37 nM and 49 nM for human, rabbit, rat, hamster and mouse neutrophil elastase, respectively.

体内研究

Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID50 = 82 pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which are induced by human neutrophil elastase.
Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats.
Sivelestat (15, 60 mg/kg, ip) prevents ischemia–reperfusion injury in the rat bladder.

Animal Model: Male Golden hamsters, weighing 90 to 110 g.
Dosage: 0.021-2.1 mg/kg.
Administration: Intratracheally five min before HNE injection.
Result: Significantly and dosedependently suppressed the lung hemorrhage.
Animal Model: Male Sprague-Dawley rats weighing 350-400 g.
Dosage: 10 mg/kg.
Administration: Continuous infusion via the tail vein at 10 mg/kg/h for 60 min during the resuscitation phase.
Result: Greatly suppressed lung injury, as revealed by the reduced histological damage.
Significantly ameliorated HSR-induced lung injury.
Markedly decreased the levels of TNF-α and iNOS gene.
Animal Model: Male Sprague Dawley rats, 8 weeks old and weighing 250-320 g.
Dosage: 15 mg/kg or 60 mg/kg.
Administration: IP.
Result: Decreased the blood flow in the bladder during reperfusion phase compared to the IR group.
分子式
C20H29N2NaO11S
分子量
528.51
CAS号
201677-61-4
中文名称
西维来司钠四水合物
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (473.03 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8921 mL 9.4606 mL 18.9211 mL
5 mM 0.3784 mL 1.8921 mL 3.7842 mL
10 mM 0.1892 mL 0.9461 mL 1.8921 mL
*

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.73 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.94 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.94 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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