Table 1.
IC50 and Ki values for compounds 4, 7-13 against iNOS
Compound | IC50(μM)a | Ki(μM)b |
---|---|---|
4 (L-NIO) | 8.1 | 3.65 |
7 | 0.4 | 0.18 |
8 | 16.1 | 7.25 |
9 | 19.1 | 8.61 |
10 | 138 | 65.18 |
11 | 68.7 | 30.95 |
12 | 323 | 146 |
13 | 5333 | 2402 |
The apparent IC50 values are represented as the mean from two or more independent experiments performed in duplicate with five or six data points each and correlation coefficients of 0.92-0.99. The experimental standard deviations were less than 10%.
The apparent Ki values were obtained by measuring the percent enzyme inhibition in the presence of 10 μM l-arginine with at least five concentrations of inhibitor. The parameters of the following inhibition equation42 were fitted to the initial velocity data: % inhibition = 100[I]/([I]+Ki(1+[S]/Km)). Km value for l-arginine was 8.2 μM (iNOS).