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  1. GPCR/G Protein
  2. Leukotriene Receptor
  3. Montelukast sodium

Montelukast sodium  (Synonyms: 孟魯司特鈉; MK0476)

目錄號: HY-13315 純度: 99.84%
COA 產(chǎn)品使用指南 技術(shù)支持

Montelukast sodium (MK0476) 是一種有效的、選擇性和具有口服活性的半胱氨酸白三烯受體 1 (CysLT1) 拮抗劑。Montelukast sodium 可用于研究預(yù)防哮喘和肝損傷。Montelukast sodium 在腸缺血-再灌注損傷中也具有抗氧化作用,還可以減少心臟損傷。Montelukast sodium 減少嗜酸性粒細(xì)胞浸潤到哮喘氣道。Montelukast sodium 也可用于 COVID-19 的研究。

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Montelukast sodium Chemical Structure

Montelukast sodium Chemical Structure

CAS No. : 151767-02-1

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥660
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50 mg ¥600
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100 mg ¥1100
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500 mg ¥2750
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1 g   詢價(jià)  
5 g   詢價(jià)  

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Customer Review

Other Forms of Montelukast sodium:

查看 Leukotriene Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Montelukast sodium (MK0476) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast sodium decreases eosinophil infiltration into the asthmatic airways. Montelukast sodium can also be used for COVID-19 research[1][2][3][4].

IC50 & Target[1]

CysLT1

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
0.31 μM
Compound: Singulair
Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
[PMID: 26985325]
HEK293 IC50
27 μM
Compound: Singulair
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
[PMID: 26985325]
體外研究
(In Vitro)

Montelukast (5 μM; 1 h) inhibits APAP (Acetaminophen) (HY-66005)-induced cell damage[1].
Montelukast (0.01-10 μM; 30 min) diminishes the 5-oxo-ETE–induced cell migration and modulates the activation of the plasmin-plasminogen system[3].
Montelukast (10 μM; 18 h) modulates the activation of MMP-9[3].

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

Cell Migration Assay [3]

Cell Line: Eosinophils
Concentration: 0.01-10 μM
Incubation Time: 30 min
Result: Diminished the 5-oxo-ETE–induced cell migration.

Western Blot Analysis[3]

Cell Line: Eosinophils
Concentration: 10 μM
Incubation Time: 18 h
Result: Reduced the 5-oxo-ETE–boosted MMP-9 secretion.
體內(nèi)研究
(In Vivo)

Montelukast (3 mg/kg; oral gavage) protects against APAP-induced hepatotoxicity in mice[1].
Montelukast (1 mg/kg; miniosmotic pump administration) reduces the airway remodeling changes observed in OVA-treated mice and blocks the actions of cysteinyl leukotrienes (LT) C4, D4, and E4 mediated by the CysLT1 receptor[2].
Montelukast (1 mg/kg; miniosmotic pump administration) reduces the elevated levels of IL-4 and IL-13 found in the BAL fluid of OVA-treated mice[2].

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

Animal Model: C57BL/6J mice (8-week-old; 22-25 g) are induced acute hepatic injury[1]
Dosage: 3 mg/kg
Administration: Oral gavage 1 h after saline or APAP administration
Result: Decreased serum levels of alanine transaminase (ALT) and aspartate aminotransferase (AST), and alleviated liver damage.
Clinical Trial
分子量

608.17

Formula

C35H35ClNNaO3S

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

孟魯司特鈉

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 50 mg/mL (82.21 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

H2O 中的溶解度 : ≥ 50 mg/mL (82.21 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.6443 mL 8.2214 mL 16.4428 mL
5 mM 0.3289 mL 1.6443 mL 3.2886 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?jiān)?年內(nèi)使用。

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實(shí)驗(yàn):

以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑: PBS

    Solubility: 1 mg/mL (1.64 mM); 懸濁液; 超聲助溶 (<60°C)

  • 方案 二

    請依序添加每種溶劑: 50% PEG300    50% Saline

    Solubility: 25 mg/mL (41.11 mM); 澄清溶液; 超聲助溶

動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
該產(chǎn)品水溶性佳,請具體參考實(shí)測 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
純度 & 產(chǎn)品資料

純度: 99.84%

參考文獻(xiàn)

Montelukast sodium 相關(guān)分類

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.6443 mL 8.2214 mL 16.4428 mL 41.1069 mL
5 mM 0.3289 mL 1.6443 mL 3.2886 mL 8.2214 mL
10 mM 0.1644 mL 0.8221 mL 1.6443 mL 4.1107 mL
15 mM 0.1096 mL 0.5481 mL 1.0962 mL 2.7405 mL
20 mM 0.0822 mL 0.4111 mL 0.8221 mL 2.0553 mL
25 mM 0.0658 mL 0.3289 mL 0.6577 mL 1.6443 mL
30 mM 0.0548 mL 0.2740 mL 0.5481 mL 1.3702 mL
40 mM 0.0411 mL 0.2055 mL 0.4111 mL 1.0277 mL
50 mM 0.0329 mL 0.1644 mL 0.3289 mL 0.8221 mL
60 mM 0.0274 mL 0.1370 mL 0.2740 mL 0.6851 mL
80 mM 0.0206 mL 0.1028 mL 0.2055 mL 0.5138 mL

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

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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Montelukast sodium
目錄號:
HY-13315
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