Biochem/physiol Actions

Reversible: no

Target IC₅₀: 42 µM against Ins(1,4,5)P3-induced Ca2+ release from rat cerebellar microsomal preparations

Product does not compete with ATP.

Primary TargetIns(1,4,5)P3-induced Ca2+ release

Cell permeable: yes

General description

A 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.

A 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. Does not affect Ca²⁺ release from the ryanodine-sensitive Ca²⁺ store in rat leg skeletal muscle and heart. Inhibits spontaneous as well as the phasic contractions induced by uterotonic agents. Also reported to inhibit angiotensin II-induced contractions in aortic muscles.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Brooke, R. T., et al. 2004. Lab. Invest.84, 29.Gregory, R.B., et al. 2001. Biochem. J.354, 285.Ma, H.T., et al. 2001. J. Biol. Chem.276, 18888.Ascher-Landsberg, S., et al. 1999. Biochem. Biophys. Res. Commun.264, 979.Maruyama, T., et al. 1997. J. Biochem.122, 498.

Packaging

100 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.

Warning

Toxicity: Standard Handling (A)