sst2

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

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

Paltusotine is a nonpeptide, small molecule somatostatin type 2 (SST2) receptor agonist with high oral bioavailability. Paltusotine maintains GH and IGF-1 levels in acromegaly patients

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.

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.

L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, demonstrating over 280-fold selectivity compared to other growth inhibitory receptors. L-803087 induces AMPA-mediated synaptic responses in the hippocampus in vitro and increases seizures in alginate-induced seizure-busting mice in vivo.

Pasireotide pamoate is a stable cyclohexapeptide somatostatin mimic. Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.

Pasireotide is a stable cyclohexapeptide somatostatin mimic.

TC-G1003 is an effective agonist of the somatostatin sst2 receptor.

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

AP-102 is a bioactive chemical.

Cortistatin-29 is a neuropeptide that is structurally similar to somatostatin-28. It is produced by cleavage of preprocortistatin to procortistatin, which is cleaved at dibasic amino acids to form cortistatin-29 and cortistatin-14 as well as other partial cleavage products. Cortistatin mRNA is expressed in the human brain and in interneurons of the rat hippocampus and cerebral cortex. Cortistatin-29 binds to somatostatin (SST) receptors with IC50 values of 2.8, 7.1, 0.2, 3, and 13.7 nM for SST1-5, respectively. Cortistatin-29 is found at similar levels as cortistatin-14 in mouse AtT20 cells but is secreted at a lower level. Cortistatin-29 corresponds to residues 85-112 of the rat peptide sequence.

L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice.

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].

Veldoreotide (DG3173) TFA, a somatostatin analogue, effectively binds to and activates somatostatin receptors (SSTR) 2, 4, and 5. This compound demonstrates a higher efficacy in inhibiting growth hormone (GH) secretion in adenomas than Octreotide, showcasing its potential as a pain modulating agent [1].

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.

N-Deacetylase/N-Sulfotransferase 2 is a sulfotransferase enzyme involved in synthesizing heparin chains attached to serglycin proteoglycan within mast cells.

somatostatin sst2 receptor agonist

L-796,778 acetate is a slective somatostatin receptor agonist with IC50 of 24nM for sst3, for sst1, sst2, sst4 and sst5, IC50 is >1000nM.

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].

XY-52 (Compound 32), an ST2 (Stimulation-2) inhibitor, exhibits IC50 values of 5.68 μM and 4.59 μM in the AlphaLISA and HEK-Blue assays, respectively. It promotes proinflammatory T-cell proliferation and diminishes plasma sST2 and IFNγ biomarkers in a graft versus host disease (GVHD) mouse model [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.