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-142928
    MAT2A-IN-1
    		Inhibitor
    MAT2A-IN-1 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally high in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-1 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-1 has the potential for the research of cancer diseases (extracted from patent WO2021139775A1, compound 64).
    MAT2A-IN-1
  • HY-P3294
    Onzigolide
    		Agonist
    Onzigolide (BIM-23A760), a chimeric dopamine-somatostatin compound, shows potent agonist activity at both DA type 2 (D2R) and SST type 2 (SSTR2) receptors.
    Onzigolide
  • HY-142930
    MAT2A-IN-3
    		Inhibitor
    MAT2A-IN-3 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally high in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-3 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-3 has the potential for the research of cancer diseases (extracted from patent WO2019191470A1, compound 265).
    MAT2A-IN-3
  • HY-160176
    SSTR5 antagonist 6
    		Antagonist
    SSTR5 antagonist 6 is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with an IC50 of 24 nM. SSTR5 antagonist 6 can be used in the study of type 2 diabetes.
    SSTR5 antagonist 6
  • HY-12819
    MK-1421
    		Antagonist
    MK-1421 is a potent and selective sstr3 antagonist. MK-1421 regulates insulin secretion by binding to the sstr3. MK-1421 can be used in the research of type 2 diabetes.
    MK-1421
  • HY-P3903
    [D-Trp8,Tyr11] Somatostatin
    [D-Trp8,Tyr11] Somatostatin is an analogue of somatostatin. Somatostatin is a hormone that regulates a variety of bodily functions. DTrp8 residue can increase stability.
    [D-Trp8,Tyr11] Somatostatin
  • HY-P3897
    [Tyr12] Somatostatin 28 (1-14)
    [Tyr12] Somatostatin 28 (1-14) is an analogue of Somatostatin-28 (1-14) (HY-P1499). Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28.
    [Tyr12] Somatostatin 28 (1-14)
  • HY-142700
    SSTR4 agonist 3
    SSTR4 agonist 3 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 3 has the potential for the research of pain (extracted from patent WO2021233427A1, compound 14).
    SSTR4 agonist 3
  • HY-P3902
    [D-Trp8] Somatostatin-14
    [D-Trp8] Somatostatin-14, a tetradecapeptide, is an analog of Somatostatin more potent than the native Somatostatin.
    [D-Trp8] Somatostatin-14
  • HY-114133
    Depreotide
    		Ligand
    Depreotide is a nove tumor tarcer, can be complexed with technetium-99m (99mTc-depreotide) for optimal imaging properties. 99mTc-depreotide somatostain receptor imaging has been playing an important role in medical diagnosis research. Depreotide can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    Depreotide
  • HY-P4957
    Octreotide dimer (parallel)
    		Agonist
    Octreotide dimer parallel is a dimer parallel of Octreotide. Octreotide (HY-P0036) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue.
    Octreotide dimer (parallel)
  • HY-137273
    Sucrose octasulfate sodium
    		Activator
    Sucrose octasulfate is a component of sulfoaluminum. Sucrose octasulfate stimulates the release of somatostatin-like immunoreactivity (SLI) from the stomach by acting directly on D cells in the gastric mucosa. Sucrose octasulfate exerts its ulcer-healing effect by releasing endogenous gastric somatostatin Sucrose octasulfate can be used for anti-gastric ulcer research .
    Sucrose octasulfate sodium
  • 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-111615
    J-2156
    		Agonist
    J-2156 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 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.
    J-2156
  • 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
    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-P10741
    DOTA-EB-TATE
    		Activator
    DOTA-EB-TATE is composed of SST peptide derivative, DOTA-octreotate conjugated a common to an Evans blue analog (EB). DOTA-EB-TATE is a peptide drug conjugate (PDC) improves the pharmacokinetics of SSTR2 analogs and reduces PRRT toxicity. DOTA-EB-TATE can also be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA-EB-TATE
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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