rKaliotoxin-1

貨號 Cat. No.
RTK-370
規格 Size
5 μg 5x5 μg 10μg 5x10μg 0.1mg

Description

rKaliotoxin-1


A Powerful Blocker of Certain Kv1and KCa1.1 Channels











Product#: RTK-370

























Sizes:
5 mg
5 x 5 mg
10 mg
5 x 10 mg
0.1 mg
 














M.W.: 4022










Sequence: GVEINVKCSG SPQCLKPCKD AGMRFGKCMN RKCHCTPK









NMR structure of Kaliotoxin (1KTX).


6,7 Kaliotoxin belongs to the a-KTX-3.1 scorpion toxin family.2










Purity: >99%












Bioassay:

Inhibition of K


V1.3 channels expressed in Xenopus oocytes by rKaliotoxin-1.











Left: Time course of current amplitude upon 250 nM rKaliotoxin-1 application and wash. Oocytes were held at ?00mV holding potential using two electrode voltage clamp. Currents were elicited by 100 ms test pulse to 0 mV, delivered every 10  seconds. Inhibition was completely reversible. Toxin was applied at the period indicated by the horizontal bar.


Middle: Traces of current response before (red) and during application of 250 nM toxin.


Right: Dose response curve for K


V1.3 channels inhibition. Each point represents 2-4 experiments as mean and S.D.







 









References:


































1.



Crest, M. et al. (1992) J. Biol. Chem. 267, 1640.



2.


Rodriguez de la Vega, R.C. and Possani, L.D. (2004), Toxicon 43, 865.

3.


Mourre, C. et al. (1999) J. Pharmacol. Exp .Ther. 291, 943.

4.


Grissmer, S. et al. (1994) Mol. Pharmacol. 45, 1227.

5.



Hopkins, W.F. et al. (1996) Curr. Pharmaceut. Design. 2, 389.



6.



Gairi, M. et al. (1997) J. Pept. Sci. 3, 314.



7.



Fernandez, I. et al. (1994) Biochemistry 33, 14256.




Kaliotoxin-1 is 38 amino acid long toxin, originally isolated from the venom of the scorpion Androctonus mauretanicus mauretanicus and is classified as a-KTX 3.1 scorpion toxin family, having three disulfide bridges.1,2 Kaliotoxin-1 is a potent inhibitor of large conductance Ca2+ -activated K+ channels (KCa1.1), and to bind and inhibit Dendrotoxin sensitive voltage-dependent K+ channels, mainly Kv1.1, Kv1.2 and Kv1.3 (KCNA1 KCNA2 and KCNA3) with Kd of 1.5, 25 and 0.1nM, respectively.1,3,4,5


 

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