(2-Aminoethoxy)(diphenyl)boran Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
Beschreibung
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.
Chemische Eigenschaften
white crystalline powder
Verwenden
Ca release inhibitor, angiogensin II inhibitor
Definition
ChEBI: An organoboron compound that is diphenylborane in which the borane hydrogen is replaced by a 2-aminoethoxy group.
Allgemeine Beschreibung
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.
Biologische Aktivität
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.
(2-Aminoethoxy)(diphenyl)boran Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
