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AS105

Chemical Structure : AS105

CAS No.: 1026029-18-4

AS105 (AS-105)

货号: PC-72972Not For Human Use, Lab Use Only.

AS105 (AS-105) is a highly potent, ATP-competitive CaMKII inhibitor, inhibits CaMKIIδ with IC50 of 8 nM, Ki of 3 nM.

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纯度 & COA & 质检文件 纯度: 99.9% (HPLC) Select Batch:

生物&药学活性

AS105 (AS-105) is a highly potent, ATP-competitive CaMKII inhibitor, inhibits CaMKIIδ with IC50 of 8 nM, Ki of 3 nM.
AS105 is also effective against autophosphorylated CaMKII (in contrast to the commonly used allosteric CaMKII-inhibitor KN-93).
In isolated atrial cardiomyocytes from human donors and ventricular myocytes from CaMKIIδC-overexpressing mice with heart failure, AS105 effectively reduced diastolic SR Ca2+ leak by 38% to 65% as measured by Ca2+-sparks or tetracaine-sensitive shift in [Ca2+]i.
AS105 effectively reduced SR Ca2+-leak, thus improving SR Ca2+-accumulation and reducing cellular arrhythmogenic correlates, without negatively influencing excitation-contraction coupling.

物理化学性质&存储条件

分子量 339.827
分子式 C18H18ClN5
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 (3.4 mg/mL)

Chemical Name/SMILES

N1-(3-(2-((3-chlorophenyl)amino)pyrimidin-4-yl)phenyl)ethane-1,2-diamine

参考文献

1. Stefan Neef, et al. J Mol Cell Cardiol. 2018 Feb;115:73-81.

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