MK571

製品コードS8126 バッチS812601

印刷

化学情報

Synonyms

L-660711

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₆H₂₇ClN₂O₃S₂

分子量

515.09

CAS No.

115104-28-4

Solubility (25°C)*

体外

DMSO

100 mg/mL (194.14 mM)

Ethanol

19 mg/mL (36.88 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (9.71mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.410mg/ml (0.80mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	MK571 is a selective, orally active CysLT1 receptor(Cysteinyl leukotriene receptor) antagonist.
in vitro	L-660,711 inhibited [3H]LTD4 binding in guinea pig lung with a Ki value of 0.22±0.15 nM (n=35) and [3H]LTD4 binding in human lung with a Ki value of 2.1±1.8 nM (n=29). L660,711 was essentially inactive versus [3H]LTC4 binding with IC50 values of 23±11 μM (n=16) and 32 μM (n=1) in guinea pig and human lung, respectively^[1].
in vivo	MK-571 is well tolerated in healthy young men. After oral administration, MK-571 is rapidly absorbed. The maximum plasma concentration occurring at 1.1-1.5 h at all doses^[3].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Glioblastoma cell lines(U251, MZ-256, and MZ-327)
	濃度	25 µM
	反応時間	7 h
	実験の流れ	Cells were seeded onto 96 well plates at a concentration of 1×10^₃ cells per well and incubated for 72 h at 37℃ and 5% CO2 to allow MRP1 messenger RNA suppression to occur. Cells were then treated with either control media or one of three chemotherapy drugs. Cells were then returned to the incubator for a further 72 h; after which time, Metylthiazol Tetrazolium (MTT) powder in PBS (50µl of 5 mg/ml) was added to each well. Cells were then incubated for a further 4 h after which all solution was removed and DMSO was added. After 10 min incubation time at 37◦C, absorbance was recorded at 570 nm wavelength and data was recorded and analyzed. Small molecule inhibitors MK571 (25 µM) and Reversan (15µM) were added 7 h prior to carrying out further drug treatment or assay assessment (media change for proliferation and 2D-migration assays)
動物実験	動物モデル	Male Msueley strain guinea pigs
	投薬量	0.001-3.0 mg/kg
	投与方法	i.v.

参考

https://pubmed.ncbi.nlm.nih.gov/2540892/
https://pubmed.ncbi.nlm.nih.gov/26136652/
https://pubmed.ncbi.nlm.nih.gov/1451725/

https://pubmed.ncbi.nlm.nih.gov/12065434/

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カスタマーフィードバック

: Data from [Data independently produced by , , Eur J Pharm Sci, 2017, 106:313-327]

: Data from [Data independently produced by , , Exp Hematol, 2017, 52:65-71]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。