Iberiotoxin
Iberiotoxin is a 37 amino acid peptidyl toxin isolated from the scorpion Mesobuthus tamulus and was shown to selectively block large conductance Ca2+-activated K+ channels(BKCa) in smooth muscle cells.?
In single channel recordings, iberiotoxin can reversibly block outward currents mediated by BKCa in excised membrane patches from bovine aortic smooth muscle with an IC50 value of 250 pM. It is also a noncompetitive, partial inhibitor of charybdotoxin binding in bovine aortic sarcolemmal membrane vesicles (Ki = 250 pM).?
Reference：
[1]. Galvez A, Gimenez-Gallego G, Reuben J P, 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. The Journal of Biological Chemisty, 1990, 265(19): 11083-11090.
| Physical Appearance | A white to off- |
| Storage | Desiccate at -20°C |
| M.Wt | 4230.85 |
| Cas No. | 129203-60-7 |
| Formula | C179H274N50O55S7 |
| Solubility | Soluble in H2O |
| SDF | Download SDF |
| Canonical SMILES | CC(CC1/C(O)=N/C(/C(O)=N/C/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(/C(O)=N/C/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(/C(O)=N/C/C(O)=N\C(/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(/C(O)=N\2)CCCNC(N)=N)CSSCC2/C(O)=N/C(/C(O)=N/C(C(O)=O)CCC(O)=N)CC3=CC=C(O)C=C3)CCCCN)CCCCN)CCSC)CSSCC(/N=C(O)/C( |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1,2]: | |
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Cell lines |
Rat dorsal root ganglion neurons, bladder |
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Preparation method |
Soluble to 0.70 mg/ml in sterile water. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10-100 nM |
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Applications |
Iberiotoxin (IbTX) (10-100 nM) increased the myogenic activity of bladder, but not portal vein. IbTX caused a sustained contracture of aorta. In rat dorsal root ganglion neurons, IbTx (100 nM) reduced whole-cell outward currents in 67% of small and medium size neurons. IbTx significantly prolonged the duration of action potential and increased firing frequency of afferent neurons. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Suarez-Kurtz, G. U. I. L. H. E. R. M. E., Garcia, M. L., & Kaczorowski, G. J. (1991). Effects of charybdotoxin and iberiotoxin on the spontaneous motility and tonus of different guinea pig smooth muscle tissues. Journal of Pharmacology and Experimental Therapeutics, 259(1), 439-443. [2]. Zhang, X. F., Gopalakrishnan, M., & Shieh, C. C. (2003). Modulation of action potential firing by iberiotoxin and NS1619 in rat dorsal root ganglion neurons. Neuroscience, 122(4), 1003-1011. | |