Phrixotoxin-2

貨號 Cat. No.
P-700
規格 Size
5 μg 5x5 μg 10μg 10μgx10μg 0.1mg

Description

 


Phrixotoxin-2


A Potent Blocker of Kv4 Channels










Product#: P-700






















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





Phrixotoxin-2 is a natural peptide isolated from the Phrixotrichus 

auratus Tarantula  venom and purified to homogeneity. 

Phrixotoxin-2 blocks specifically and reversibly Kv4.2 and Kv4.3 channels.1 

These channels are probably the molecular counterparts of the A-type current (Ito1) in the heart. 

Cloned Kv4.2 and Kv4.3 channels heterologously expressed in COS cell were blocked with  

IC50 of 34 and 71 nM of Phrixotoxin-2 respectively.1  








M.W.: 3921










Sequence: YCQKW MWTCD EERKC CEGLV CRLWC KRIIN M










Purity: >98%












Bioassay:
In Xenopus oocytes the toxin was less potent then in COS cells and inhibited KV4.3 with IC50 of about 650nM (see below).  

In addition the block is highly voltage dependent and is much more potent at negative potentials (see below).










KV4.3 channel currents were recorded from Xenopus oocytes using the two electrode voltage clamp, with ND 96 solution in the bath.  

Left: Traces of current response to 100 ms depolarization from holding potential of -100 mV to -10 mV,  

applied every 10s. before during and after wash of the indicated Phrixotoxin 2 concentration.  

Middle: Mean and S.D. dose-response curve for 3 experiments such as in the left.  

Right: Mean and S.D. voltage dependence of the percentage inhibition caused by 1 mM Phrixotoxin 2 (n=3).













References:










1.

Diochot, S. et al. (1999) Br. J. of Pharmacol. 126, 251.

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