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-139802
    L-779976
    		Agonist
    L-779976 is a compound with bradykinin agonist activity. Injection into the amygdala and septum of the rat brain can produce anxiolytic effects. Its bradykinin agonist activity has been verified by relevant experiments.
    L-779976
  • HY-139806
    SRA880 free base
    		Inhibitor
    SRA880 (free base) is a compound with antidepressant-modulating effects. It is a somatostatin-1 autoreceptor antagonist that can synergize with imipramine to produce antidepressant-like effects and affect BDNF mRNA expression and phosphorylation of related proteins.
    SRA880 free base
  • HY-P2229
    Ilatreotide
    Ilatreotide (SDZ CO61), glycated somatostatin derivative, is a highly potent glycated analog of somatostatin with improved oral activity. Ilatreotide can suppress the fasting level and postprandial release of several gastrointestinal and pancreatic hormones. Ilatreotide can be used for the research of gastroenteropancreatic tumors.
    Ilatreotide
  • HY-RS13834
    Sstr5 Rat Pre-designed siRNA Set A
    		Inhibitor

    Sstr5 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sstr5 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sstr5 Rat Pre-designed siRNA Set A
  • HY-RS13827
    Sstr3 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Sstr3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sstr3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sstr3 Mouse Pre-designed siRNA Set A
  • HY-172147
    SSTR4 agonist 5
    		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.
    SSTR4 agonist 5
  • HY-120287
    L-054522
    		Agonist
    L-054522 is an agonist for somatostatin receptor subtype 2 with Kd 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).
    L-054522
  • HY-P3952
    (D-Trp8,D-Cys14)-Somatostatin-14
    		Control
    (D-Trp8,D-Cys14)-Somatostatin-14 is a Somatostatin synthetic analogue. (D-Trp8,D-Cys14)-Somatostatin-14 can be used for the research of metabolic related diseases.
    (D-Trp8,D-Cys14)-Somatostatin-14
  • HY-163317
    MMC(TMZ)-TOC
    MMC(TMZ)-TOC has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC targets delivery of TMZ to SSTR2-positive tumor cells. MMC(TMZ)-TOC can be used for the research of cancer.
    MMC(TMZ)-TOC
  • HY-P11463
    Des-threoninol-octreotide
    		Inhibitor
    Des-threoninol-octreotide (Compound 13) is a Somatostatin analog. Des-threoninol-octreotide inhibits cloned somatostatin receptors with IC50 values of 13.62 nM, 10.63 nM, 10.95 nM for mSSTR2b, rSSTR5 and hSSTR5, respectively.
    Des-threoninol-octreotide
  • HY-P11485
    JR11-PEG3-HBED-CC-PSMA-03
    		Antagonist
    JR11-PEG3-HBED-CC-PSMA-03 (Compound 1) is an RDC-related compound containing the chelating agent HBED-CC, the JR11 peptide (SSTR2 antagonist), and the PSMA ligand. JR11-PEG3-HBED-CC-PSMA-03 shows SSTR2-binding affinities and PSMA-binding affinities, with IC50 s of 59.2 nM, 57.0 nM, respectively. JR11-PEG3-HBED-CC-PSMA-03 can be radiolabeled with [68Ga]. [68Ga] radiolabeled JR11-PEG3-HBED-CC-PSMA-03 can be used in diagnostic studies of neuroendocrine differentiated prostate cancer.
    JR11-PEG3-HBED-CC-PSMA-03
  • HY-RS13826
    SSTR3 Human Pre-designed siRNA Set A
    		Inhibitor

    SSTR3 Human Pre-designed siRNA Set A contains three designed siRNAs for SSTR3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SSTR3 Human Pre-designed siRNA Set A
  • HY-RS13831
    Sstr4 Rat Pre-designed siRNA Set A
    		Inhibitor

    Sstr4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sstr4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sstr4 Rat Pre-designed siRNA Set A
  • HY-142929
    MAT2A-IN-2
    		Inhibitor
    MAT2A-IN-2 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-2 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-2 has the potential for the research of cancer diseases (extracted from patent WO2020243376A1, compound 172).
    MAT2A-IN-2
  • HY-RS13825
    Sstr2 Rat Pre-designed siRNA Set A
    		Inhibitor

    Sstr2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sstr2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sstr2 Rat Pre-designed siRNA Set A
  • HY-RS13833
    Sstr5 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Sstr5 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sstr5 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sstr5 Mouse Pre-designed siRNA Set A
  • 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)
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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