Iberiotoxin

Iberiotoxin; 纯度: ge;95.0%

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。

Iberiotoxinamp;;

Iberiotoxin Chemical Structure

CAS No. : 129203-60-7

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生物活性

Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca2+-activated K+ channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels[1][2][3].

IC50 Target

Kd: 1 nM (Ca2+-activated K+ channel)[1][3]

体外研究
(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[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

4230.85

Formula

C179H274N50O55S7

CAS 号

129203-60-7

Sequence

Glp-Phe-Thr-Asp-Val-Asp-Cys-Ser-Val-Ser-Lys-Glu-Cys-Trp-Ser-Val-Cys-Lys-Asp-Leu-Phe-Gly-Val-Asp-Arg-Gly-Lys-Cys-Met-Gly-Lys-Lys-Cys-Arg-Cys-Tyr-Gln (Disulfide bridge:Cys7-Cys28,Cys13-Cys33,Cys17-Cys35)

Sequence Shortening

{Glp}-FTDVDCSVSKECWSVCKDLFGVDRGKCMGKKCRCYQ (Disulfide bridge:Cys7-Cys28,Cys13-Cys33,Cys17-Cys35)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
参考文献
  • [1]. A Galvez, et al. Purification and Characterization of a Unique, Potent, Peptidyl Probe for the High Conductance Calcium-Activated Potassium Channel From Venom of the Scorpion Buthus Tamulus. J Biol Chem. 1990 Jul 5;265(19):11083-90.

    [2]. Santiago Echeverry, et al. Activation of BK Channel Contributes to PL-Induced Mesenchymal Stem Cell Migration. Front Physiol. 2020 Mar 24;11:210.

    [3]. S Candia, et al. Mode of Action of Iberiotoxin, a Potent Blocker of the Large Conductance Ca(2+)-activated K+ Channel. Biophys J. 1992 Aug;63(2):583-90.

    [4]. R J Wang, et al. Downregulation of Large Conductance Calcium-Activated Potassium Channels in Paraventricular Nucleus Contributes to Sympathoexcitation in Rats With Chronic Heart Failure. Zhonghua Xin Xue Guan Bing Za Zhi. 2018 Mar 24;46(3):178-186.