2-APB (2-Aminoethyl Diphenylborinate)

製品コードS6657 バッチS665701

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。

1.400mg/ml (6.22mM) Taking the 1 mL working solution as an example, add 50 μL of 28 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。

1.400mg/ml (6.22mM) Taking the 1 mL working solution as an example, add 50 μL of 28 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.[3]

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.[4]

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 (2-Aminoethyl Diphenylborinate) being included among these agents. 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/

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:

Ageing-Dependent Thyroid Hormone Receptor α Reduction Activates IP3R1-Meditated Ca2+ Transfer in MAM and Exacerbates Skeletal Muscle Atrophy in Mice [ Cell Prolif, 2025, e70120.] PubMed: 40851314
Calcium-mediated mitochondrial fission and mitophagy drive glycolysis to facilitate arterivirus proliferation [ PLoS Pathog, 2025, 21(1):e1012872] PubMed: 39804926
Reactive Oxygen Species-Mediated TRPM2 Activation Facilitates Phagocytosis of Macrophages to Reverse Profibrotic Phenotype [ Liver Int, 2025, 45(10):e70341] PubMed: 40952323
Pentatrichomonas hominis induces extracellular traps formation of macrophages via the TLR2/NADPH/PAD4 pathway [ Parasit Vectors, 2025, 18(1):248] PubMed: 40598534
Matrix stiffness aggravates osteoarthritis progression through H3K27me3 demethylation induced by mitochondrial damage [ iScience, 2024, 27(8):110507] PubMed: 39156637
Mild therapeutic hypothermic protection activates the PI3K/AKT signaling pathway to inhibit TRPM7 and suppress ferroptosis induced by myocardial ischemia‑reperfusion injury [ Mol Med Rep, 2024, 30(6)220] PubMed: 39364741
Porcine reproductive and respiratory syndrome virus infection triggers autophagy via ER stress-induced calcium signaling to facilitate virus replication [ PLoS Pathog, 2023, 19(3):e1011295] PubMed: 36972295
Only one carbon difference determines the pro-apoptotic activity of α-tocopheryl esters [ FEBS J, 2022, 10.1111/febs.16623] PubMed: 36083714
Overexpression of Rhodopsin or Its Mutants Leads to Energy Metabolism Dysfunction in 661w Cells [ Invest Ophthalmol Vis Sci, 2022, 63(13):2] PubMed: 36469028
Endophilin A2-mediated alleviation of endoplasmic reticulum stress-induced cardiac injury involves the suppression of ERO1α/IP3R signaling pathway [ Int J Biol Sci, 2021, 17(13):3672-3688] PubMed: 34512174

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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