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首页-小分子抑制剂&激动剂-Cytoskeleton/Cell Adhesion Molecules-Myosin-CK-586
CK-586

Chemical Structure : CK-586

CAS No.: 2830607-59-3

CK-586 (CK-4021586, CK586)

货号: PC-22762Not For Human Use, Lab Use Only.

CK-4021586 (CK-586) is a potent, selective and oral cardiac myosin inhibitor, inhibits the ATPase activity of two-headed heavy meromyosin (HMM) but not single-headed subfragment-1.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CK-4021586 (CK-586) is a potent, selective and oral cardiac myosin inhibitor, inhibits the ATPase activity of two-headed heavy meromyosin (HMM) but not single-headed subfragment-1.
CK-586 is a partial inhibitor of cardiac myofibrillar ATPase activity (EC50=2.9 µM) that requires the regulatory light chain.
In preclinical models, CK-586 reduced cardiac hypercontractility by decreasing the number of active myosin cross-bridges during cardiac contraction thereby reducing the contractile force, without effect on calcium transients.

物理化学性质&存储条件

分子量 405.45
分子式 C21H25F2N3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2,5,8-Triazaspiro[3.5]nonane-2-carboxaldehyde, 5-[(3,4-difluorophenyl)methyl]-8-(trans-4-methylcyclohexyl)-6,9-dioxo-

参考文献

1. Victor N Rivas, et al. Sci Rep. 2024 May 27;14(1):12038.

2. Saswata Sankar Sarkar, et al. Biophys J, VOLUME 122, ISSUE 3, SUPPLEMENT 1, 122A, FEBRUARY 10, 2023

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