SSTR2 Agonist

Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.

Ac-crown-TATE is an actinium-labeled radioligand derived from the SSTR2 agonist crown-TATE, which targets neuroendocrine tumors with high SSTR2 expression. The [226Ac]Ac-crown-TATE form of Ac-crown-TATE possesses both SPECT-detectable γ-emission and α-radiation properties, and it inhibits tumor growth and prolongs survival. Ac-crown-TATE can be used in studies of SSTR2-positive neuroendocrine tumors, targeted α-radiation, and radionuclide imaging.

BIM-23190 hydrochloride, a somatostatin analog, a selective SSRT2 and SSRT5 agonist, exhibits K_i values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly.

Veldoreotide (DG3173) TFA a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide TFA inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent

Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst₂/sst₅ receptor partial agonist with IC₅₀ values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research.

BIM-23197 is a selective SST2 (IC₅₀ = 0.19 nM) agonist. BIM-23197 can effectively stimulate intracellular calcium mobilization in cells expressing SST2. BIM-23197 can be used for research on endocrine related conditions.

BIM-23190, a somatostatin analog, a selective SSTR2 and SSTR5 agonist, exhibits K_i values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly.

Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.

sst2 Receptor agonist-1 is a potent somatostatin receptor subtype 2 (sst₂) agonist with a K_i value of 0.025 nM and a cAMP IC₅₀ value of 4.8 nM. sst2 Receptor agonist-1 can inhibit rat growth hormone (GH) secretion and ocular neovascular lesion formation. Antiangiogenic effect.

Angiopeptin, a cyclic octapeptide analogue of somatostatin, is a weak sst₂/sst₅ receptor partial agonist with IC₅₀ values of 0.26 nM and 6.92 nM, respectively. Angiopeptin is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin has the potential for coronary atherosclerosis research.

Onzigolide (BIM-23A760), a chimeric dopamine-somatostatin compound, shows potent agonist activity at both DA type 2 (D2R) and SST type 2 (SSTR2) receptors.