Atpenin A5 是高度特异性的complex II抑制剂,IC50为 ~10 nM。DolaSTATin 10也是有效的mKATP通道激动剂,具有心脏保活的作用。
产品描述
Atpenin A5 is a potent and highly specific complex II inhibitor (IC50 ~10 nM). Atpenin A5 is also an effective mKATP channel agonist and cardioprotective agent[1].
体外活性
Atpenin A5 shows the inhibition profile for submitochondrial particles (SMPs), mitochondria, and cardiomyocytes, with IC50 values of 8.3 nM, 9.3 nM, and 8.5 nM, respectively. Atpenin A5 (AA5) is a potent and specific complex II inhibitor. Atpenin A5 (1 nM) also activates the mKATP channel and protects against simulated ischemia-reperfusion (IR) injury in isolated cardiomyocytes[1].
体内活性
Atpenin A5 is a potent inhibitor of succinate dehydrogenase (SDH). SDH inhibition by Atpenin A5 promotes cardiomyocyte mitosis and regeneration in the postnatal heart after myocardial infarction (MI). Atpenin A5-injected (100 μg/kg) mice demonstrated myocardial thickness at the infarct zone and a significant reduction in scar size compared with controls[2].
Cas No.
119509-24-9
分子式
C15H21Cl2NO5
分子量
366.24
储存和溶解度
DMSO:100 mg/mL (273.04 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years