2-Aminoethoxydiphenyl borate

개요2-Aminoethyl diphenylborinate (2-APB) is a modulator of intracellular calcium levels and transient receptor potential (TRP) channels. It inhibits calcium release induced by inositol-1,4,5-triphosphate (IP3) in rat cerebellar microsomes (IC50 = 42 μM) without affecting IP3 binding to its receptor. 2-APB inhibits store-operated calcium entry (SOCE) in DT40 cells (IC50 = 4.8 μM), as well as inhibits TRP canonical 6 (TRPC6) and TRP melastatin 8 (TRPM8) and activates TRP vanilloid 1 (TRPV1), TRPV2, and TRPV3 in vitro. It also inhibits calcium transients induced by the sarcoplasmic/endoplasmic reticulum Ca2+-ATPase (SERCA) inhibitor thapsigargin in DDT1 MF-2 cells when used at a concentration of 75 μM. 2-APB inhibits differentiation of primary mouse brown adipocytes when used at concentrations ranging from 30 to 300 μM and reduces adipocyte triglyceride levels at 100 μM. It also increases the expression of Ucp1 and Pparg in primary mouse brown adipocytes. 2-APB (10 mg/kg) reduces protein levels of TRP melastatin 2 (TRPM2) in the rat hippocampus and improves learning and memory deficits induced by amyloid-β (25-35) in rats.

용도Ca release inhibitor, angiogensin II inhibitor

일반 설명A cell-permeable modulator of Ins(1,4,5)P3-induced Ca2+ release. Inhibits Ins(1,4,5)P3-induced Ca2+ release from rat cerebellar microsomal preparations (IC50 = 42 μM) without affecting [3H]-Ins(1,4,5)P3 binding to its receptor. In liver cells, 2-APB inhibits store-operated Ca2+ channels through a mechanism which may involve its binding to either the channel protein or an associated regulatory protein. Has no effect on the Ca2+ release from the ryanodine-sensitive Ca2+ store prepared from rat leg skeletal muscle and heart.