EIPA (L593754)

製品コードS9849 バッチS984901

印刷

化学情報

 Chemical Structure Synonyms L593754; MH 12-43 Storage
(From the date of receipt)
3 years -20°C powder
化学式

C11H18ClN7O

分子量 299.76 CAS No. 1154-25-2
Solubility (25°C)* 体外 DMSO 60 mg/mL (200.16 mM)
Ethanol 30 mg/mL (100.08 mM)
Water 2 mg/mL (6.67 mM)
* <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 EIPA (L593754; MH 12-43) acts as an inhibitor of macropinocytosis and sodium-hydrogen exchangers(NHE) (IC50=0.033μg/mL). EIPA blocks the activity of Na(+)/H(+) exchanger, which are plasma membrane proteins implicated in all forms of macropinocytosis.
in vitro

This compound rapidly and reversibly block Ca2+-activated TRPP3 channel activation, with IC50s of 10.5 μM.

in vivo

EIPA downregulates endothelial cell activation of NF-kappaB and VCAM-1 expression and attenuates the early inflammatory stages of atherogenesis and stent intimal formation.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Xenopus laevis oocyte
濃度 100 μM
反応時間 30 min
実験の流れ

The uptake of radioactive 45Ca2+ mediated by TRPP3 channel  is tested using the standard NaCl-containing solution, plus 1 mM nonradiolabeled CaCl2 and radiolabeled 45Ca2+ in the presence and absence of 100 μM EIPA. Control uptake level is obtained using H2O-injected oocytes.

動物実験 動物モデル Murine Model of Atherogenesis (apoE-/- mice)
投薬量 3 mg/kg
投与方法 s.c.

参考

  • https://pubmed.ncbi.nlm.nih.gov/24184990/
  • https://pubmed.ncbi.nlm.nih.gov/17804601/
  • https://pubmed.ncbi.nlm.nih.gov/15505102/

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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。

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