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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，K_d 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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