CAS | 209006-18-8 |
Sequence | H-p-Chloro-Phe-D-Cys-β-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2 (Disulfide bond) |
Sequence Single | p-Chloro-Fc-β-(3-pyridyl)-AwK-tBu-GC-2-Nal-NH2 |
Molecular Formula | C59H71ClN12O8S2 |
Molecular Weight | 1175.87 |
Technology | Synthetic |
Storage | -20°C, avoid light, cool and dry place |
Description | PRL2915, H-p-Chloro-Phe-D-Cys-β-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2 (Disulfide bond), highly potent human somatostatin subtype 2 receptor (hsst2) antagonist with a Ki of 12 nM. Ki values for the other subtypes were >1000 nM for hsst1, 100 ± 57 nM for hsst3, 895 nM for hsst4, and 520 nM for hsst5, respectively. No agonist activity was found when tested alone at concentrations up to 10 µM. In a rat pituitary growth hormone in vitro antagonist assay versus somatostatin-14 (1nM) the somatostatin octapeptide analog PRL2915 exhibited an IC50 value of 1.8 nM. |
References | 1. A novel Abeta isoform pattern in CSF reflects gamma-secretase inhibition in Alzheimer disease. E.Portelius et al., Alzheimer Res. Ther., 2, 7 (2010) |