Table 1 Stimulation of purified sGC in the presence and absence of DTT by the NO donor SNP. YC-1 and the ortho-. meta- and para-PALs with Mg2+ as cofactor. Shown are the x-fold stimulations versus basal specific activity of SNP (1 μM). YC-1 (100 μM, 10 μM, 1 μM and 1 μM YC-1 in combination with 1μM SNP) and the different PALs (100 μM, 10 μM, 1 μM and 1 μM PAL in combination with 1 μM SNP). The data presented represent the mean ± SEM out of four independent experiments performed in duplicate.
From: NO-independent regulatory site of direct sGC stimulators like YC-1 and BAY 41-2272
Stimulation of purified sGC [fold increase vs. basal activity ± SEM] (basal specific activity [nmol/mg/min]) | |||
|---|---|---|---|
Stimulator | Concentration | + DTT | -DTT |
Basal | 1.0 ± 0.1 (64 ± 8) | 1.0 ± 0.2 (150.8 ± 33.4) | |
SNP | 1 μM | 82.3 ± 10.5 | 17.1 ± 2.2 |
100 μM | 45.9 ± 7.7 | 44.4 ± 4.8 | |
YC-1 | 10 μM | 4.5 ± 0.8 | 7.0 ± 1.7 |
1 μ M | 2.0 ± 0.4 | 1.5 ± 0.2 | |
YC-1 + SNP | 1 μM + 1 μM | 98.4 ± 17.3 | 20.6 ± 3.6 |
100 μM | 14.4 ± 1.6 | 21.4 ± 4.2 | |
ortho-PAL | 10 μM | 2.9 ± 1.5 | 3.1 ± 0.6 |
1 μ M | 2.1 ± 1.0 | 1.0 ± 0.1 | |
ortho-PAL + SNP | 1 μM + 1 μM | 85.7 ± 11.4 | 15.8 ± 2.0 |
100 μM | 54.7 ± 10.2 | 56.1 ± 0.1 | |
meta-PAL | 10 μM | 21.3 ± 7.1 | 23.3 ± 4.1 |
1 μ M | 4.5 ± 1.0 | 4.9 ± 0.4 | |
meta-PAL + SNP | 1 μM + 1 μM | 185.6 ± 72.6 | 39.0 ± 5.6 |
100 μM | 36.6 ± 3.5 | 30.2 ± 4.5 | |
para-PAL | 10 μM | 15.3 ± 2.7 | 17.3 ± 1.9 |
1 μM | 3.5 ± 0.4 | 3.8 ± 0.3 | |
para-PAL + SNP | 1 μM + 1 μM | 229.1 ± 33.6 | 50.6 ±5.5 |