2-APB (2-Aminoethyl Diphenylborinate)

製品コードS6657 バッチS665703

印刷

化学情報

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

C14H16BNO

分子量 225.09 CAS No. 524-95-8
Solubility (25°C)* 体外 DMSO 45 mg/mL (199.92 mM)
Ethanol 23 mg/mL (102.18 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 40%PEG300 5%Tween80 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。

1.100mg/ml (4.89mM) Taking the 1 mL working solution as an example, add 50 μL of 22 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 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。

0.750mg/ml (3.33mM) Taking the 1 mL working solution as an example, add 50 μL of 15 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 2-APB (2-Aminoethyl Diphenylborinate) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations.
in vitro

2-APB (2-Aminoethyl Diphenylborinate), an inositol 1, 4, 5-trisphosphate receptor (IP3R) inhibitor, obviously attenuates the intracellular Ca2+ release and cardiomyocyte apoptosis induced by oxygen and glucose deprivation (OGD) stimulation and EndoA2 knockdown.

in vivo

2-APB (2-Aminoethyl Diphenylborinate) increases the basilar artery (BA) wall thickness and reduced the BA lumen diameter, inducing significant vascular changes, also alleviates cell apoptosis at 24 hours after SAH.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 neonatal rat cardiomyocytes
濃度 2 h
反応時間 --
実験の流れ

Neonatal Sprague-Dawley rats (1 to 3 days old) are exposed to hypothermia until they became unresponsive and are then euthanized by cervical dislocation. Primary culture of NRCMs is performed. The cells are seeded at a density of 5 x 106 cells/ml in Dulbecco's modified Eagle's medium supplemented with 10% fetal bovine serum and 0.1 mM 5-bromodeoxyuridine. After 24 h, NRCMs are subjected to various treatments as described below. To assess the effects of EndoA2 on cardiac injury, the cells are transfected with EndoA2 siRNA or Ad-EndoA2. After transfection for 36 h, the cells are stimulated with oxygen and glucose deprivation (OGD) for another 12 h. Incubation of 4-Phenylbutyric acid (4-PBA), Cyclosporin A (CsA), 1,2-bis(o-aminophenoxy)ethane-N,N,N ,N -tetraacetic acid (BAPTA) or 2-Aminoethoxydiphenylborate (2-APB) is 2 h before OGD stimulation, with this compound being 2-Aminoethyl Diphenylborinate. Cardiomyocytes are cultured in serum-free, glucose and sodium pyruvate-free DMEM at 37 ℃ in an anoxia chamber saturated with 94% N2/5% CO2/ 1% O2.

動物実験 動物モデル Rats of subarachnoid hemorrhage (SAH) model
投薬量 0.5, 2 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/11162848/
  • https://pubmed.ncbi.nlm.nih.gov/23040501/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8416715/
  • https://pubmed.ncbi.nlm.nih.gov/30905651/

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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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