Table 1.
Stability, H2S release, and vasodilating activity of H2S donors.
Compd 1 | Stability and H2S Release In Human Serum |
Vasodilating Activity | ||||
---|---|---|---|---|---|---|
% Compd (at 1, 4, 24 h) ± SE or Half-Life |
% H2S mol/mol (at 1, 4, 24 h) Hours ± SE |
EC50 (μM) ± SEM [% Vasodilation] |
+ Glib. 10 μM EC50 (μM) ± SEM [% Vasodilation] |
|||
1 | 88 ± 1 | 1 h | 0.4 ± 0.1 | 1 h | NA | NA |
35 ± 1 | 4 h | 1.5 ± 0.1 | 4 h | |||
8.0 ± 0.5 | 24 h | 3.9 ± 0.9 | 24 h | |||
2 | t1/2 < 30 min | 0.6 ± 0.3 | 1 h | NA | NA | |
1.8 ± 0.3 | 4 h | |||||
5 ± 1 | 24 h | |||||
3 | 80.0 ± 1.0 | 1 h | 1.5 ± 0.2 | 1 h | NA | NA |
62 ± 2 | 4 h | 8.2 ± 0.3 | 4 h | |||
44 ± 1 | 24 h | 23 ± 2 | 24 h | |||
4 | t1/2 < 30 min | 5.8 ± 0.2 | 1 h | 64 ± 6 | [44 ± 3] 2 | |
10 ± 1 | 4 h | |||||
24.2 ± 0.9 | 24 h | |||||
5 | 64 ± 1 | 1 h | 2.7 ± 0.2 | 1 h | [16 ± 4] 3 | |
39 ± 1 | 4 h | 11 ± 2 | 4 h | |||
16 ± 1 | 24 h | 21 ± 1 | 24 h | |||
6 | t1/2 < 30 min | 5.8 ± 0.2 | 1 h | 47 ± 8 | [34 ± 7] 2 | |
10 ± 1 | 4 h | |||||
24.2 ± 0.8 | 24 h | |||||
7 | 19.8 ± 0.7 | 1 h | 0.3 ± 0.2 | 1 h | [12 ± 1] 3 | |
0 | 4 h | 1.4 ± 0.2 | 4 h | |||
0 | 24 h | 5 ± 1 | 24 h | |||
8 | t1/2 < 30 min | 16 ± 1 | 1 h | 40 ± 3 | 40 ± 4 | |
25.8 ± 0.4 | 4 h | |||||
47 ± 1 | 24 h | |||||
9 | 94.2 ± 0.2 | 1 h | 0.4 ± 0.1 | 1 h | 78 ± 7 | 262 ± 62 |
90.0 ± 0.8 | 4 h | 1.7 ± 0.6 | 4 h | |||
83 ± 1 | 24 h | 4.4 ± 0.9 | 24 h | |||
10 | t1/2 = 2.4 h | 1.8 ± 0.3 | 1 h | [29 ± 3] 4 | ||
7.5 ± 0.6 | 4 h | |||||
12.0 ± 0.9 | 24 h | |||||
11 | 96.3 ± 0.2 | 1 h | 0.4 ± 0.4 | 1 h | [42 ± 3] 2 | |
90.0 ± 0.9 | 4 h | 4 ± 1 | 4 h | |||
53 ± 2 | 24 h | 33 ± 4 | 24 h | |||
12 | t1/2 = 2.7 h | 17 ± 8 | 1 h | 20 ± 2 | 20 ± 3 | |
63 ± 30 | 4 h | |||||
146 ± 34 | 24 h | |||||
13 | 99.2 ± 0.1 | 1 h | 0 | 1 h | [39 ± 8] 2 | |
96.0 ± 0.8 | 4 h | 0.7 ± 0.2 | 4 h | |||
94.3 ± 2 | 24 h | 2.4 ± 0.5 | 24 h | |||
14 | t1/2 = 30 min | 0 | 1 h | [37 ± 3] 4 | ||
0.5 ± 0.3 | 4 h | |||||
1.8 ± 0.6 | 24 h | |||||
15 | 99.2 ± 0.1 | 1 h | 0.2 ± 0.4 | 1 h | [17 ± 3] 3 | |
95 ± 1 | 4 h | 1.3 ± 0.2 | 4 h | |||
94.8 ± 2 | 24 h | 2.8 ± 0.5 | 24 h | |||
16 | t1/2 = 1.5 h | 0.4 ± 0.2 | 1 h | [25 ± 5] 2 | ||
1.7 ± 0.5 | 4 h | |||||
2.5 ± 0.9 | 24 h | |||||
17 | 91.6 ± 0.3 | 1 h | 0.2 ± 0.2 | 1 h | [27 ± 6] 3 | |
85.0 ± 0.1 | 4 h | 1.0 ± 0.3 | 4 h | |||
64.7 ± 0.2 | 24 h | 6 ± 1 | 24 h | |||
18 | t1/2 = 3.7 h | 1.4 ± 0.4 | 1 h | [33 ± 6] 4 | ||
11.0 ± 0.3 | 4 h | |||||
44 ± 2 | 24 h |
1 Compound. 2 Percent vasodilation at the maximum concentration testable (100 μM). 3 Percent vasodilation at the maximum concentration testable (300 μM). 4 Percent vasodilation at the maximum concentration testable (10 μM).