Iberiotoxin (trifluoroacetate salt) |
| Catalog No.GC43886 |
Iberiotoxin (trifluoroacetate salt) is a selective high conductance high conductance Ca2+-activated K+ channel inhibitor with a Kd of ~1 nM. Iberiotoxin (trifluoroacetate salt) does not block other types of voltage-dependent ion channels.
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Cas No.: 182897-30-9
Sample solution is provided at 25 µL, 10mM.
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Iberiotoxin (trifluoroacetate salt) is a selective high conductance high conductance Ca2+-activated K+ channel inhibitor with a Kd of ~1 nM. Iberiotoxin (trifluoroacetate salt) does not block other types of voltage-dependent ion channels[1，2，3].
Iberiotoxin (trifluoroacetate salt) treatment affects rat mesenchymal stem cells (rMSCs) migration in the absence of platelet lysate (PL) by inducing a decrease in cell migration. 10 nM of Iberiotoxin (trifluoroacetate salt) abolishes the PL-induced migration effect on MSCs[3]. Iberiotoxin (trifluoroacetate salt) reversibly blocks Ca2+-activated K+ channel in excised membrane patches from bovine aortic smooth muscle. Iberiotoxin (trifluoroacetate salt) acts exclusively at the outer face of the channel and functions with IC50 values of about 250 pM[1].
Male Wistar rats (6-7 weeks old) with chronic heart failure (CHF), after perfusion of Iberiotoxin (trifluoroacetate salt), right ventricular weight/body weight and lung weight/body weight ratio as well as left ventricular end-diastolic diameter were increased and left ventricular ejection fraction was decreased, the sympathetic driving indexes was increased in sham rats, changes of these parameters further aggravated in CHF rats. In rats, Downregulation and blunted function of BKCa by Iberiotoxin (trifluoroacetate salt) in PVN may contribute to sympathoexcitation and deterioration of cardiac function in rats with chronic heart failure[4].BK channels were expressed in mouse lymphatic smooth muscle and Iberiotoxin (trifluoroacetate salt) (BK channel inhibitors) produced right-ward shifts in NONOate concentration-response curves[5].BKCa channels localize to the mitochondria of adult mouse[6], rat ventricular cardiomyocytes present and plasma membrane of neonatal cardiomyocytes,Inhibition of BKCa channels by Iberiotoxin (trifluoroacetate salt) protects neonatal hearts against myocardial ischemia and reperfusion injury[7]. Iberiotoxin (trifluoroacetate salt) as a blocker of KCa1.1 channels, inhibited acetylcholine relaxation in corpus cavernosum from db/+ mice, while there was no effect in tissue from db/db mice[8].
References:
[1]: Galvez A, Gimenez-Gallego G, 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. PMID: 1694175.
[2]: Echeverry S, Grismaldo A, et,al. Activation of BK Channel Contributes to PL-Induced Mesenchymal Stem Cell Migration. Front Physiol. 2020 Mar 24;11:210. doi: 10.3389/fphys.2020.00210. PMID: 32265729; PMCID: PMC7105713.
[3]: Candia S, Garcia ML, 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. doi: 10.1016/S0006-3495(92)81630-2. PMID: 1384740; PMCID: PMC1262182.
[4]: Wang RJ, Wen ML, 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. Chinese. doi: 10.3760/cma.j.issn.0253-3758.2018.03.003. PMID: 29562421.
[5]: Kim HJ, Li M, et,al. Large-conductance calcium-activated K+ channels, rather than KATP channels, mediate the inhibitory effects of nitric oxide on mouse lymphatic pumping. Br J Pharmacol. 2021 Oct;178(20):4119-4136. doi: 10.1111/bph.15602. Epub 2021 Aug 7. PMID: 34213021.
[6]: Frankenreiter S, Bednarczyk P, et,al. cGMP-Elevating Compounds and Ischemic Conditioning Provide Cardioprotection Against Ischemia and Reperfusion Injury via Cardiomyocyte-Specific BK Channels. Circulation. 2017 Dec 12;136(24):2337-2355. doi: 10.1161/CIRCULATIONAHA.117.028723. Epub 2017 Oct 19. PMID: 29051185.
[7]: Sanghvi S, Szteyn K, et,al. Inhibition of BKCa channels protects neonatal hearts against myocardial ischemia and reperfusion injury. Cell Death Discov. 2022 Apr 7;8(1):175. doi: 10.1038/s41420-022-00980-z. PMID: 35393410; PMCID: PMC8989942.
[8]: Comerma-Steffensen S, Prat-Duran J, et,al. Erectile Dysfunction and Altered Contribution of KCa1.1 and KCa2.3 Channels in the Penile Tissue of Type-2 Diabetic db/db Mice. J Sex Med. 2022 May;19(5):697-710. doi: 10.1016/j.jsxm.2022.02.021. Epub 2022 Mar 20. PMID: 35321830.
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