Somatostatin Receptors

Octreotide is a peptide agonist for sst2, sst3 and sst5 somatostatin receptors. IC50/Kd values (nM) at cloned human somatostatin receptors are: 290 - 1140 (sst1), 0.4 - 2.1 (sst2), 4.4 - 34.5 (sst3), > 1000 (sst4), and 5.6 - 32 (sst5).

Somatostatin is an endogenous peptide noted to inhibit the release of growth hormone, insulin and glucagon.

CYN-154806 is a potent selective somatostatin receptor 2 (sst2) antagonist.

Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).

Octreotide is a somatostatin analog that binds to the somatostatin receptor, mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production.

SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM).

SSTR5 antagonist 1 is a potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively. (Compound 25a).

Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).

MK-4256 is a potent and selective SSTR3 antagonist with IC50s of 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively.

SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM).

DOTA-JR11 is a somatostatin receptor 2 (SSTR2) antagonist. DOTA-JR11 can be labeled by 68Ga, used for paired imaging in neuroendocrine tumors (NETs) research.