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Iberiotoxin
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Iberiotoxin
CAS No. : 129203-60-7
MCE 站:Iberiotoxin
产品活性:Iberiotoxin 是一种从 Buthus tamulus 毒液中分离出来的毒素。Iberiotoxin 是一种选择性的高电导率 Ca2+ 激活的 K+ 通道 (Ca2+-activated K+ channel) 抑制剂,Kd 约为 1 nM。Iberiotoxin 不阻断其他类型的电压依赖性离子通道。
研究领域:Membrane Transporter/Ion Channel
作用靶点:Potassium Channel
In Vitro: Iberiotoxin reversibly blocks Ca2+-activated K+ channel in excised membrane patches from bovine aortic smooth muscle. Iberiotoxin acts exclusively at the outer face of the channel and functions with IC50 values of about 250 pM. Iberiotoxin is a partial inhibitor of 125I-charybdotoxin binding in bovine aortic sarcolemmal membrane vesicles (Ki of 250 pM). Iberiotoxin functions as a noncompetitive inhibitor of charybdotoxin binding.
Iberiotoxin treatment affects rat mesenchymal stem cells (rMSCs) migration in the absence of platelet lysate (PL) by inducing a decrease in cell migration suggesting that BK channels regulate rMSCs migration in basal conditions. 10 nM of Iberiotoxin abolishes the PL-induced migration effect on MSCs.
In Vivo: Male Wistar rats (6-7 weeks old) with chronic heart failure (CHF), Iberiotoxin (0.125 nmol/nl, 1.25 nmol/nl and 12.5 nmol/nl) is infused into paraventricular hypothalamic nucleus (PVN) by osmotic minipumps. After perfusion of Iberiotoxin by microinjection of rAAV2-KCNMB4 shRNA virus, right ventricular weight/body weight and lung weight/body weight ratio as well as left ventricular end-diastolic diameter are increased and left ventricular ejection fraction is decreased.
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