Skip to main content
. 2000 Nov 28;97(25):13973–13978. doi: 10.1073/pnas.250483897

Table 1.

Chemical characteristics and sst1-5 binding affinity of sst3-selective and control peptides

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.