Table 1.
ID no. | Compound | Purity
|
MS
|
IC50,*
nM
|
||||||
---|---|---|---|---|---|---|---|---|---|---|
HPLC | CZE | Calc. | Found | sst 1 | sst 2 | sst 3 | sst 4 | sst 5 | ||
1 | SS-28 | >98 | >98 | 3147.5 | 3147.7 | 3.9 ± 0.3 (19) | 3.3 ± 0.2 (22) | 7.1 ± 0.7 (21) | 3.8 ± 0.3 (22) | 3.9 ± 0.3 (20) |
2 | Cortistatin | 96 | >98 | 1720.8 | 1720.9 | 3.9 ± 1.5 (4) | 4.6 ± 0.4 (3) | 6.8 ± 1.6 (3) | 2.5 ± 0.5 (3) | 13 ± 3.1 (4) |
3 | des-AA1,2,4,5,12,13[d-Trp8]-SS (ODT-8) | >94 | 98 | 1079.5 | 1079.2 | 28 ± 4.7 (3) | 44 ± 13 (4) | 13 ± 4 (3) | 1.3 ± 0.8 (3) | 45 ± 27 (3) |
4 | des-AA1,2,4,5,12,13[d-2Nal8]-SS (ODN-8) | >98 | 98 | 1090.5 | 1090.5 | 607 ± 167 (3) | 173 ± 41 (3) | 6.7 ± 1.9 (3) | 56 ± 22 (3) | 28 ± 15 (3) |
5 | des-AA1,2,4,5,12,13[dAgl8(2-naphthoyl)]-SS | >98 | >98 | 1119.5 | 1119.4 | >10,000 (4) | >10,000 (5) | >1,000 (4) | 165 ± 45 (3) | >10,000 (4) |
6 | des-AA1,2,4,5,12,13[d-Agl8(Me,2-naphthoyl)]-SS | 98 | >98 | 1133.5 | 1133.6 | >10,000 (4) | >10,000 (6) | 70 ± 17 (5) | >10,000 (3) | >10,000 (4) |
7 | des-AA1,2,4,5,12,13[d-Cys3, d-Agl8(Me,2-naphthoyl)]-SS | >98 | 98 | 1133.5 | 1133.5 | >10,000 (5) | >10,000 (4) | 115 ± 36 (4) | >10,000 (4) | >1,000 (4) |
8 | des-AA1,2,4,5,12,13[Tyr7, d-Agl8(Me,2-naphthoyl)]-SS | >98 | 98 | 1149.5 | 1149.2 | >10,000 (5) | >10,000 (5) | 70 ± 18 (4) | >1,000 (5) | >10,000 (4) |
9 | des-AA1,2,4,5,12,13[d-Cys3,Tyr7, d-Agl8(Me,2-naphthoyl)]-SS | >98 | >98 | 1149.5 | 1149.3 | >10,000 (7) | >10,000 (7) | 39 ± 11 (6) | >10,000 (7) | >10,000 (6) |
10 | Carbamoyl-des-AA1,2,4,5,12,13[d-Cys3, Tyr7, d-Agl8(Me,2-naphthoyl)]-SS (sst3-ODN-8) | >98 | — | 1192.4 | 1192.4 | >10,000 (3) | >10,000 (3) | 6.7 ± 2.6 (3) | >10,000 (3) | >10,000 (3) |
11 | L-796-778 | 585.7 | >10,000 (3) | >10,000 (3) | 127 ± 31 (4) | >10,000 (3) | >10,000 (3) |
SS, somatostatin-14; SS-28, somatostatin-28; MS, mass spectrum as [mass + H]+; CZE, capillary zone electrophoresis.
Mean ± SEM. Number of experiments in parentheses.