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-16381B
    Pasireotide (diaspartate)
    		Agonist
    Pasireotide (SOM230) diaspartate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide diaspartate exhibits antisecretory, antiproliferative, and proapoptotic activity.
    Pasireotide (diaspartate)
  • HY-P3314
    Nendratareotide
    Nendratareotide is a somatostatin analogue.
    Nendratareotide
  • HY-P2090
    Angiopeptin
    		Agonist
    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.
    Angiopeptin
  • HY-P2150
    Cortistatin-29 (rat)
    Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects.
    Cortistatin-29 (rat)
  • 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-177278
    SST1 receptor antagonist-1
    		Antagonist
    SST1 receptor antagonist-1 (Compound 23) is a selective Somatostatin receptor 1 (SST1) antagonist with pKds of 9.11 and 8.79 for rSST1 and hSST1, respectively. SST1 receptor antagonist-1 can be used for retinal and endocrine dysfunctions, cancer and neuropsychiatric disorders research.
    SST1 receptor antagonist-1
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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