AP102 is a dual SSTR2/SSTR5-specific somatostatin analog (SSA). AP102 is a disulfide-bridged octapeptide SSA containing synthetic iodinated amino acids. AP102 binds with subnanomolar affinity to SSTR2 and SSTR5 (IC50: 0.63 and 0.65 nM, respectively). AP102 does not bind to SSTR1 or SSTR3. AP102 can be used for acromegaly and neuroendocrine tumors research[1].
in vivo
AP102 (0-30 μg/kg, sc) acutely reduces growth hormone but does not cause hyperglycemia during acute or chronic administration in a healthy rat model[1].
IC 50
SSTR2: 0.63 nM (IC50); SSTR5: 0.65 nM (IC50)
References
[1] Tarasco E, et al. Effect of AP102, a subtype 2 and 5 specific somatostatin analog, on glucose metabolism in rats. Endocrine. 2017 Oct;58(1):124-133. DOI:10.1007/s12020-017-1386-2
