Somatostatin Receptor Agonist

SSTR4 agonist 5 (Compound 5) is the orally active agonist for somatostatin receptor 4 (SSTR4) with an EC₅₀ of 0.228 nM. SSTR4 agonist 5 exhibits good stability in human/rat liver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models.

L-054522 is an agonist for somatostatin receptor subtype 2 with K_d of 0.01 nM. L-054522 inhibits growth hormone release from rat primary pituitary cell (IC₅₀=0.05 nM) and glucagon and insulin release from isolated mouse pancreatic islet cell (IC₅₀=0.05 nM and 12 nM).

Pasireotide (SOM230) diaspartate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide diaspartate exhibits antisecretory, antiproliferative, and proapoptotic activity.

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.

SSTR3 agonist-1 TFA is a potent, orally active, and selective SSTR3 agnoist (EC₅₀ =0.14 nM). SSTR3 agonist-1 TFA binds to SSTR3 receptor to inhibit cAMP activity. SSTR3 agonist-1 TFA decreases kidney weight and kidney cystic index (KCI) in a mouse model of autosomal dominant polycystic kidney disease (ADPKD). SSTR3 agonist-1 TFA can be used for ADPKD research.

Octreotide dimer parallel is a dimer parallel of Octreotide. Octreotide (HY-P0036) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue.

Pasireotide (aspartate) TFA, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide (aspartate) TFA can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide (aspartate) TFA also exhibits antisecretory, antiproliferative, and proapoptotic activity.

Cyclic SSTR agonist octreotide is a Octreotide (HY-P0036), serving as the cyclic Somatostatin Receptor SSTR agonist.

L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a K_i of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.

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.

L-797591 is a selective sst₁ agonist. L-797591 mimicks the effects of SRIF-14 and SRIF-28 by potently inhibiting either Forskolin (HY-15371)-stimulated or CRH-stimulated cAMP accumulation.

L-803087 (Standard) is the analytical standard of L-803087 (HY-108497). This product is intended for research and analytical applications. L-803087 is a potent and selective somatostatin sst4 receptor agonist with a K_i of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.

Octreotide-d₈ (SMS 201-995-d₈) is deuterium labeled Octreotide. 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.

Branosotine (compound 1-1) is a potent agonist of somatostatin receptor (SSTR2), with the EC₅₀ of ＜0.1 nM.

Zavolosotine (Compound 1) is an orally active agonist for somatostatin receptor type 5 (SST5) with EC₅₀ <1 nM. Zavolosotine inhibits insulin and glucagon secretion, increases levels of glucagon in blood in rat model.

Mazisotine (CNTX-0290) tartrate is an orally active, non-opioid somatostatin receptor 4 (SSTR4) agonist with an EC₅₀ of 4.7 nM. Mazisotine tartrate exerts significant analgesic effects in various nociceptive (inflammatory, osteoarthritic) and neuropathic pain models. Mazisotine tartrate can be used for pain research.

J-2156 TFA (Standard) is the analytical standard of J-2156 (TFA) (HY-111615A). This product is intended for research and analytical applications. J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC₅₀s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.