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Merck
CN

5.31547

RyR1 Modulator, CCDI

别名:

RyR1 Modulator, CCDI, Ryanodine Receptor 1 Modulator

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关于此项目

经验公式（希尔记法）:
C18H25N3O
分子量:
299.41
UNSPSC Code:
12352200

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assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

off-white

solubility

DMSO: 100 mg/mL

Quality Level

100

General description

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).
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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
RyR1

Preparation Note

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

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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