sst2

Pasireotide (SOM230) acetate is a long-acting cyclohexapeptide growth hormone inhibitory hormone analog with antisecretory, antiproliferative, and proapoptotic activities.Pasireotide (SOM230) acetate inhibits the secretion of GH, IGF-I, and ACTH, and can be used in the study of acromegaly and Cushing's disease. Pasireotide (SOM230) acetate also enhances the agonist activity of growth inhibitory receptors, with pKi of 8.2, 9.0, 9.1, <7.0 and 9.9 for sst1, 2, 3, 4 and 5, respectively.

Cortistatin-14, a neuropeptide structurally similar to growth inhibitor-14, has anticonvulsant and neuroprotective effects and impairs recognition memory consolidation in mice through activation of sst(2), growth hormone-releasing peptide, and GABA(A B) receptor, which can be used to study sepsis-induced cognitive impairment.

Angiopeptin is a synthetic octapeptide analog of somatostatin; suppresses accelerated transplant atherosclerosis in rabbit heart arteries.

Seglitide acetate (MK-678) is a selective agonist of sst2 somatostatin receptor.

AP-102 is a bioactive chemical.

BIM-23190 aceate, a somatostatin analog, a selective agonist of SSTR2 and SSTR5. BIM-23190 can be used in cancer and acromegaly studies.

Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, acts as a partial agonist at sst 2 sst 5 receptors, with IC50 values of 0.26 nM and 6.92 nM, respectively. It effectively inhibits the release of growth hormone and the production of insulin-like growth factor-1 (IGF-1), and either inhibits adenylate cyclase activity or promotes extracellular acidification. Angiopeptin TFA shows promise for use in coronary atherosclerosis research [1] [2].

PRL 2915 is a potent antagonist of the human somatostatin subtype 2 receptor (hsst 2), exhibiting a binding affinity (K_i) of 12 nM [1].

PRL 3195 is a somatostatin receptor antagonist with K i values of 6, 17, 66, 1000, and 1000 nM for human somatostatin receptors sst 5, sst 2, sst 3, sst 1, and sst 4, respectively [1].

BIM-23027 is a selective sst 2 receptor agonist (EC 50 = 0.32 nM) with effects analogous to the cyclic tetradecapeptide somatostatin (SRIF). It promotes dopamine release through a Glu-dependent mechanism [1] [2].

CYN 154806 TFA is a cyclic octapeptide and an effective selective somatostatin sst2 receptor antagonist. For the recombinant sst2, sst1, sst3, sst4 and sst5 receptors, the pIC50 values are 8.58, 5.41, 6.07, 5.76 and 6.48, respectively.

CYN 154806 is a potent and selective somatostatin sst2 receptor antagonist, The pIC50 values are 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.

Potent somatostatin receptor 1 (sst1) agonist; displays selectivity for sst1 (IC50 values are 30.9 nM, 345 nM, > 1 μM, > 10 μM and > 10μM for human sst1, sst3, sst4, sst2 and sst5 respectively). Attenuates somatostatin release in the rat nucleus accumbens

Peptide agonist for sst2 and sst5 somatostatin receptors. IC50/Kd values (nM) at cloned human somatostatin receptors are: > 1000 (sst1), 0.2 - 1.5 (sst2), 27 - 36 (sst3), > 127 (sst4), and 0.06 - 23 (sst5).

Veldoreotide, also known as Somatoprim, is a unique somatostatin receptor subtypes 2-, 4- and 5-selective analogue which effectively reduces GH secretion in human GH-secreting pituitary adenomas, even in Octreotide non-responsive tumours.