rErgtoxin-1

貨號 Cat. No.
RTE-450
規格 Size
5 μg 5x5 μg 10μg 5x10μg 0.1mg

Description

 


rErgtoxin-1

A Novel ERG1 (Kv11.1) K+ Channel Blocker









Product#: RTE-450






















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














M.W.: 4730










Sequence:
DRDSC VDKSR CAKYG YYQEC QDCCK NAGHN GGTCM FFKCK CA











Purity: >98%












Bioassay:

Potent inhibition of Kv11.1 (hERG) K+ Channels by rErgtoxin-1.













Effects of rErgtoxin-1 on Kv11.1 (hERG) in two-electrode voltage clamp of Xenopus oocytes (above).

Application of rErgtoxin-1 inhibits the current amplitude in a concentration dependent (see figures A and B, IC50 of 60 nM) and reversible manner. The block spanned the voltage range of these channels activity (figure C).

A. hERG channel currents (in 5 mM K+) elicited by 500 ms depolarization from holding potential of  -100 mV to +20 mV, before and during application of rErgtoxin-1 of the indicated concentration.  

B. Mean ?S.D. dose response for rErgtoxin-1 block of hERG channels (n was between 2-7 oocytes for each point).  

C. Mean ?S.D. I-V relation of control and inhibited currents (n=4).













 

Top: Example traces of KV11.1 currents elicited with the voltage protocol that is illustrated below, for control currents and increasing toxin concentrations (details in the inset).

Bottom: Dose response for the toxin effect in these cells (n=4-7 for each data point, IC50 of about 5 nM).

Effects of rErgtoxin-1 on KV11.1 (hERG) channels stably expressed in HEK-293 cells using whole cell patch clamp recording (above).













References:














1.

Scaloni, A. et al. (2000) FEBS Lett, 479, 156.  

2.

Gurrola, G.B. et al. (1999) FASEB. J. 13, 953.  


Ergtoxin-1 was originally isolated from Centruroides noxius scorpion venom. rErgtoxin-1 is a recombinant peptide

expressed in and extracted from E. coli and purified to homogeneity.  

Ergtoxin-1 blocks specifically Kv11.1 (ERG) K+ channels in different tissues and across species.2  

Patch clamp recordings from cultured cell lines and cardiac myocytes showed specific block of ERG  

currents with IC50 of 16 nM, and increase firing-rate in neurons as well as cardiac action potential broadening.2

 

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