JNJ 303 是有效的IKs阻断剂,IC50为 64 nM。它浓度在 3.3 μM 时对其他心脏通道无任何影响。它诱导 QT 延长并引起无端尖端扭转型室性心动过速。
产品描述
JNJ 303 is a potent blocker of IKs (IC50 : 64 nM).
体外活性
Optical mapping was used to measure action potential durations (APDs) in the presence of the IKs blocker JNJ-303 and the IKr blocker E-4031.?JNJ-303 alone did not increase APD.?However, under isoprenaline (ISO), both the application of JNJ-303 and additional E-4031 significantly increased APD.?With JNJ-303, ISO decreased APD significantly more in the epicardium as compared to the endocardium, with subsequent application E-4031 increasing mid- and endocardial APD80 more significantly than in the epicardium.?We found that β-AR stimulation significantly augmented the effect of IKs blocker JNJ-303, in contrast to the reduced effect of IKr blocker E-4031[1].
Cas No.
878489-28-2
分子式
C21H29ClN2O4S
分子量
440.98
别名
JNJ 303
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years