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. Author manuscript; available in PMC: 2014 Jun 29.
Published in final edited form as: ChemMedChem. 2009 Mar;4(3):406–414. doi: 10.1002/cmdc.200800292

Table 1.

Comparison of the kinetics parameters of KIIIA and it disulfide-deficient analogs in blocking NaV1.2 and NaV1.4

Analog NaV1.2 NaV1.4
%[a] Block kobs
(min-1)
koff
(min-1)
kon [b]
(μM•min)-1
Kd [c]
(μM)
% Block kobs
(min-1)
koff
(min-1)
kon [b]
(μM•min)-1
Kd [c]
(μM)
KIIIA 90±3 0.36±0.06 0.0016±0.0016 0.36±0.06 0.004±0.004 86±6 0.91±0.17 0.05±0.017 0.86±0.17 0.06±0.02
KIIIA[C1A, C9A] 93±2 1.8±0.39 0.014±0.002 1.8±0.39 0.008±0.002 85±2 4.0±0.5 0.78±0.1 3.22±0.51 0.24±0.05
KIIIA[C2A, C15A] 66±4 0.07±0.02 0.01±0.0014 0.06±0.02 0.17±0.06 71±4 0.56±0.08 0.15±0.03 0.41±0.09 0.37±0.11
KIIIA[C4A, C16A] 8±3 n.a. [d] n.a. -- -- 1±1 n.a. n.a. -- --
[a]

Percent block was determined at steady-state or plateau value of single exponential fit of time course of block during 20 min. of exposure to 1 μM peptide;

[b]

kon was estimated from {kobs – koff};

[c]

Kd was estimated from {koff/kon};

[d]

n.a., unable to be determined because level of block was too small. Values represent mean s.d. from at least three different oocytes.