2-Aminoethyl diphenylborinate

2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of Inositol triphosphate receptor (IP3R). 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca²⁺ (SOC) channel and activates some TRP channels (V1, V2 and V3). Additionally, 2-Aminoethyl diphenylborinate has inhibitory effects on vasospasm. At high concentrations, it exhibits specific anti-inflammatory and antioxidant effects in neural tissue^{[1][2][3][4][5]}. IC50 & Target:Inositol triphosphate receptor (IP3R) In Vitro:2-Aminoethyl diphenylborinate (2-APB) (10-100 μM, 2 min) evokes external acid-dependent increases of [Ca²⁺] and dopamine release in PC12 cells through the activation of Orai 3^[3].
2-Aminoethyl diphenylborinate (100 μM, 9 h) provides protective effects against ischemia-reperfusion (I/R)-induced damage in Hep G2 cells^[5].
In Vivo:2-Aminoethyl diphenylborinate (0.5 or 2 mg/kg, i.p., administered for 24 hours) exhibited an inhibitory effect on vasospasm in Sprague-Dawley rats^[2].
2-Aminoethyl diphenylborinate (2 or 4 mg/kg, i.p., single administration for 10 min) reduces the oxidative stress and apoptosis caused by testicular ischemia-reperfusion injury in rats^[4].
2-Aminoethyl diphenylborinate (2 mg/kg, i.v. (via portal vein), 10 min before ischemia) is effective in preventing hepatic Ischemia-reperfusion (I/R) damage when administered via the portal vein before ischemiain an in mice model of liver Ischemia-reperfusion (I/R) injury^[5].