Bosentan

製品コードS4220 バッチS422002

印刷

化学情報

Synonyms

Ro 47-0203

Storage
(From the date of receipt)

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

化学式

C₂₇H₂₉N₅O₆S

分子量

551.61

CAS No.

147536-97-8

Solubility (25°C)*

体外

DMSO

100 mg/mL (181.28 mM)

Ethanol

16 mg/mL (29.0 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 (9.06mM)	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。	2.500mg/ml (4.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 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	Bosentanは、ET-AおよびET-Bのエンドセリン（ET）受容体アンタゴニストであり、K_iはそれぞれ4.7 nMおよび95 nMです。
in vitro	In vitro, bosentan has been shown to improve human endothelial cell and reduce neointimal and smooth muscle proliferation.
in vivo	In pigs in vivo, bosentan has been shown to partially restore hypoxia-induced reductions in nitric oxide.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Human Hepatocytes
	濃度	1, 10 and 100 µM
	反応時間	24 h
	実験の流れ	Incubation solutions containing bosentan (1, 10 and 100 µM) are prepared in cell culture medium. On the sixth day of culturing of the sandwich-cultured hepatocytes, cell culture medium is removed from the wells and incubation solution containing bosentan is added to the cells. The cells were incubated with the solution for 24 h at 37°C. After the exposure, the incubation solution id removed and the cells are rinsed with Plus (+) or Minus (−) buffer. The buffer solution is then removed and the cells are incubated with fresh Plus (+) or Minus (−) buffer for 5 min at 37°C. Following this 5 minute incubation, the buffer solution is collected and any remaining buffer is removed. The cells are then washed three times with ice-cold Plus (+) buffer and the plates are frozen at −80°C until processed for bioanalysis.
動物実験	動物モデル	DSS rats, Wistar rats
	投薬量	3 to 600 mg/kg
	投与方法	oral administration

参考

https://pubmed.ncbi.nlm.nih.gov/19791841/
https://pubmed.ncbi.nlm.nih.gov/24582812/
https://pubmed.ncbi.nlm.nih.gov/21119207/

https://pubmed.ncbi.nlm.nih.gov/24498134/

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カスタマーフィードバック

: Data from [Data independently produced by , , PLoS One, 2016, 11(9): e0161988.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Acquired resistance to combination treatment through loss of synergy with MEK and PI3K inhibitors in colorectal cancer. [Bhattacharya B, et al. Oncotarget, 2016, 7(20):29187-98]	PubMed: 27081080
Stimulation of Transforming Growth Factor-β1-Induced Endothelial-To-Mesenchymal Transition and Tissue Fibrosis by Endothelin-1 (ET-1): A Novel Profibrotic Effect of ET-1 [Wermuth PJ, et al. PLoS One, 2016, 11(9):e0161988]	PubMed: 27583804

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。