ジフェニルボリン酸2-アミノエチル 化学特性,用途語,生産方法
外観
白色～褐色, 結晶性粉末～粉末
溶解性
エタノールに溶け、水にほとんど溶けない。
使用上の注意
不活性ガス封入
説明
2-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 (IP
3) in rat cerebellar microsomes (IC
50 = 42 μM) without affecting IP
3 binding to its receptor. 2-APB inhibits store-operated calcium entry (SOCE) in DT40 cells (IC
50 = 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 Ca
2+-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.
化学的特性
white crystalline powder
使用
Ca release inhibitor, angiogensin II inhibitor
定義
ChEBI: An organoboron compound that is diphenylborane in which the borane hydrogen is replaced by a 2-aminoethoxy group.
一般的な説明
A cell-permeable modulator of Ins(1,4,5)P
3-induced Ca
2+ release. Inhibits Ins(1,4,5)P
3-induced Ca
2+ release from rat cerebellar microsomal preparations (IC
50 = 42 μM) without affecting [
3H]-Ins(1,4,5)P
3 binding to its receptor. In liver cells, 2-APB inhibits store-operated Ca
2+ channels through a mechanism which may involve its binding to either the channel protein or an associated regulatory protein. Has no effect on the Ca
2+ release from the ryanodine-sensitive Ca
2+ store prepared from rat leg skeletal muscle and heart.
生物活性
A functional and membrane permeable D-myo-inositol 1,4,5-trisphosphate (IP 3 ) receptor antagonist (IC 50 = 42 μ M). Stimulates store-operated calcium (SOC) release at low concentrations (< 10 μ M) and inhibits it at higher concentrations (up to 50 μ M). Increases STIM-Orai channel conductance and limits ion selectivity. Modulator of TRP channels; blocks TRPC1, TRPC3, TRPC5, TRPC6, TRPV6, TRPM3, TRPM7, TRPM8 and TRPP2 and at higher concentrations stimulates TRPV1, TRPV2 and TRPV3. Also blocks specific gap channel subtypes.
ジフェニルボリン酸2-アミノエチル 上流と下流の製品情報
原材料
準備製品