2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Somatostatin Receptor

Somatostatin Receptor

SSTRs; SSTR

Somatostatin Receptor

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Somatostatin receptors (SSTR1, 2A and B, 3, 4 and 5) belong to the G protein coupled receptor family. Somatostatin receptors are expressed in a variety of human tumors, including most tumors of neuroendocrine origin, breast tumors, certain brain tumors, renal cell tumors, lymphomas, and prostate cancer. Somatostatin triggers cytostatic and cytotoxic effects and has a general inhibitory effect on secretion mediated through its interaction with somatostatin receptors.

The SSTRs 1-4 display weak selectivity for somatostatin-14 binding, whereas SSTR5 is somatostatin-28-selective. Based on structural similarity and reactivity for octapeptide and hexapeptide somatostatin receptor analogs, SSTRs 2, 3 and SSTR5 belong to a similar somatostatin receptor subclass; SSTRs 1-4 react poorly with these analogs and belong to a separate subclass. All five somatostatin receptors are functionally coupled to inhibition of adenylyl cyclase via pertussis toxin-sensitive guanosine triphosphate (GTP)-binding proteins. mRNA for SSTRs 1-5 is widely expressed in brain and peripheral organs and displays an overlapping but characteristic pattern that is subtype-selective and tissue- and species-specific. All pituitary cell subsets express SSTR2 and SSTR5, with SSTR5 being more abundant. Individual pituitary cells coexpress multiple somatostatin receptor subtypes.

Somatostatin Receptor Isoform Specific Products:

Somatostatin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P2434
    AP102
    AP102 is a dual SSTR2/SSTR5-specific somatostatin analog (SSA). AP102 is a disulfide-bridged octapeptide SSA containing synthetic iodinated amino acids. AP102 binds with subnanomolar affinity to SSTR2 and SSTR5 (IC50: 0.63 and 0.65 nM, respectively). AP102 does not bind to SSTR1 or SSTR3. AP102 can be used for acromegaly and neuroendocrine tumors research.
    AP102
  • HY-108501
    (1R,1'S,3'R/1R,1'R,3'S)-L-054,264
    		Agonist
    (1R,1'S,3'R/1R,1'R,3'S)-L-054,264 is a selective non-peptide human somatostatin receptor subtype 2 (sst2) agonist. (1R,1'S,3'R/1R,1'R,3'S)-L-054,264 can be used in the study of retinal neuromodulation.
    (1R,1'S,3'R/1R,1'R,3'S)-L-054,264
  • HY-RS13832
    SSTR5 Human Pre-designed siRNA Set A
    		Inhibitor

    SSTR5 Human Pre-designed siRNA Set A contains three designed siRNAs for SSTR5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SSTR5 Human Pre-designed siRNA Set A
  • HY-P3958
    BIM-23027
    		Agonist 99.76%
    BIM-23027 is a selective agonist of sst2 receptor (EC50=0.32 nM), with similar effect to somatostatin (SRIF), a cyclic tetradecapeptide. BIM-23027 stimulates dopamine release, which is mediated by a Glu-dependent mechanism.
    BIM-23027
  • HY-P4100
    Cyclic SSTR agonist octreotide
    		Agonist
    Cyclic SSTR agonist octreotide is a Octreotide (HY-P0036), serving as the cyclic Somatostatin Receptor SSTR agonist.
    Cyclic SSTR agonist octreotide
  • HY-108497A
    L-803087 TFA
    		Agonist
    L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki 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.
    L-803087 TFA
  • HY-RS13829
    SSTR4 Human Pre-designed siRNA Set A
    		Inhibitor

    SSTR4 Human Pre-designed siRNA Set A contains three designed siRNAs for SSTR4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SSTR4 Human Pre-designed siRNA Set A
  • HY-RS13823
    SSTR2 Human Pre-designed siRNA Set A
    		Inhibitor

    SSTR2 Human Pre-designed siRNA Set A contains three designed siRNAs for SSTR2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SSTR2 Human Pre-designed siRNA Set A
  • HY-123460
    BN-81674
    		Antagonist
    BN-81674 is a somatostatin analogue and a selective antagonist of the non-peptide human somatostatin sst3 receptor (Ki=0.92 nM). In addition, BN-81674 reversed the inhibition of cyclic AMP accumulation induced by 1 nM somatostatin through the sst3 receptor with an IC50 value of 0.84 nM. BN-81674 can be used in cancer research.
    BN-81674
  • HY-177282
    SST1 receptor antagonist-2
    		Antagonist
    SST1 receptor antagonist-2 (Example 2) is a piperazine derivative and a somatostatin receptor 1 (SST1) antagonist. SST1 receptor antagonist-2 can be used in the research of psychiatric diseases, neurodegenerative diseases, tumors, as well as vascular disorders and immunological diseases.
    SST1 receptor antagonist-2
  • HY-P0036S2
    Octreotide-d8
    		Agonist
    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.
    Octreotide-d<sub>8</sub>
  • HY-159825
    Branosotine
    		Agonist
    Branosotine (compound 1-1) is a potent agonist of somatostatin receptor (SSTR2), with the EC50 of ＜0.1 nM.
    Branosotine
  • HY-164040
    Zavolosotine
    		Agonist
    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.
    Zavolosotine
  • HY-139347A
    Mazisotine tartrate
    		Agonist
    SSTR4 agonist-1 tartrate (Preparation 4) is a SSTR4 agonist.
    Mazisotine tartrate
  • HY-157303
    SSTR5 antagonist 3
    		Antagonist
    SSTR5 antagonist 3 (Compound 23) is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with low hERG inhibition. SSTR5 antagonist 3 exhibits potency with IC50 values of 2.8 nM and 1.4 nM in human and mouse, respectively. SSTR5 antagonist 3 can be used for the research of anti-gallstone.
    SSTR5 antagonist 3
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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