Biochem/physiol Actions

Primary TargetRyR1

Cell permeable: yes

General description

A cell-permeable pyrrolo[1,2-c]imidazolone derived compound that selectively and preferentially binds to the cytoplasmic domain of mammalian ryanodine receptor 1 (RyR1) in a reversible manner and potentiates Ca2+-dependent binding of [3H]-ryanodine to RyR1(EC₅₀ = 6 µM). Increases the open probability (Po) of RyR1 without affecting RyR2, RyR3, or the IP3R. Does not alter RyR1 conductance or the Kd for 3H-ryanodine binding to RyR1 in any significant manner (~4 nM vs 4.2 nM with and without CCDI in the medium). Induces Ca2+ transients in C2C12 skeletal myotubes, but does not alter Ca2+ transients in rat ventricular myocytes.

A cell-permeable pyrrolo[1,2-c]imidazolone derived compound that selectively and preferentially binds to the cytoplasmic domain of mammalian ryanodine receptor 1 (RyR1) in a reversible manner and potentiates Ca2+-dependent binding of [3H]-ryanodine to RyR1(EC₅₀ = 6 µM). Increases the open probability (Po) of RyR1 without affecting RyR2, RyR3, or the IP3R. Does not alter RyR1 conductance or the Kd for 3H-ryanodine binding to RyR1 in any significant manner (~4 nM vs 4.2 nM with and without CCDI in the medium). Induces Ca2+ transients in C2C12 skeletal myotubes, but does not alter Ca2+ transients in rat ventricular myocytes.Please note that the molecular weight for this compound is batch-specific due to variable water content.

A cell-permeable compound that selectively and reversibly binds to the cytoplasmic domain of mammalian RyR1 and potentiates Ca2+-dependent binding of [3H]-ryanodine to RyR1(EC₅₀ = 6 µM).

Legal Information

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

Other Notes

Tian, C., et al. 2014. Br. J. Pharmcol.171, 4097.

Packaging

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)