MRS 2578

製品コードS2855 バッチS285501

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H20N6S4
分子量 472.67 CAS No. 711019-86-2
Solubility (25°C)* 体外 DMSO 42 mg/mL (88.85 mM)
Water Insoluble
Ethanol 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
30%propylene glycol 5%Tween80 65%D5W

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。

 30.000mg/ml (63.47mM) Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. 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 MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.
in vitro MRS2578 selectively blocks P2Y6 receptor activity versus activity at P2Y1, P2Y2, P2Y4 or P2Y11 receptors. This compound (1 μM) completely blocks the protection by UDP undergoing TNFalpha-induced apoptosis in 1321N1 astrocytoma cells. [1] It inhibits basal NF-κB activity in time and dose dependent manner in HMEC-1 cells transfected with 0.25 μg NF-κB promoter reporter. This chemical (10 μM) completely abolishes TNF-α induced NF-κB reporter activity in HMEC-1 cells. It (10 μM) significant reduces TNF-α–induced proinflammatory gene expression in HMEC-1 cells. [2] The compound potentiates ATPγS and UDP response at concentrations below 316 nM whereas above this concentration, it inhibits ATPS- and UDP-induced IP accumulation in neonatal rat cardiac myofibroblasts. [3] MRS2578-treated mice shows reduced bronchial hyperresponsiveness toward methacholine in OVA-sensitized mice. This compound completely blocks UDP-induced the release of IL-6, KC, and IL-8 in lung epithelial cells. [4]
in vivo MRS 2578 (10 μM) attenuates Keratinocyte-derived chemokine serum protein levels in LPS-induced vascular inflammation in C57BL/6 mice. [2] This compound (10 μM, intratracheally) reduces BALF eosinophilia and the levels of IL-5 and IL-13 in the BALF in OVA-sensitized mice and leads to a markedly attenuated change in methacholine responsiveness after OVA challenge. This compound (10 μM, intratracheally) inhibits house dust mite–induced allergic airway inflammation in OVA-sensitized mice. This compound (10 μM, intratracheally) reduces of IL-6 and KC levels in BALF in OVA-sensitized mice. [4]

プロトコル(参考用のみ)

動物実験 動物モデル Murine endotoxinemia model
投薬量 10 μM (100 μL)
投与方法 Intravenous injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/15081875/
  • https://pubmed.ncbi.nlm.nih.gov/21173118/
  • https://pubmed.ncbi.nlm.nih.gov/19422377/
  • https://pubmed.ncbi.nlm.nih.gov/21512170/

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：

Blocking the A2B adenosine receptor alleviates myocardial damage by inhibiting spleen-derived MDSC mobilisation after acute myocardial infarction [ Ann Med, 2022, 54(1):1616-1626] PubMed: 35675334
Adenosine deaminase modulates metabolic remodeling and orchestrates joint destruction in rheumatoid arthritis [ Sci Rep, 2021, 11(1):15129] PubMed: 34301999

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。