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

Somatostatin Receptor

SSTRs; SSTR

Somatostatin Receptor

Related Products

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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-P11488
    JR11-PEG3-DOTA-PSMA-03
    		Ligand
    JR11-PEG3-DOTA-PSMA-03 (Compound 2) is an RDC-related compound containing the chelating agent DOTA (HY-W053583), the JR11 peptide (SSTR2 antagonist), and the PSMA ligand. JR11-PEG3-DOTA-PSMA-03 shows SSTR2-binding affinities and PSMA-binding affinities, with IC50 s of 94.0 nM, 81.8 nM, respectively. JR11-PEG3-DOTA-PSMA-03 can be radiolabeled with [68Ga]. [68Ga] radiolabeled JR11-PEG3-DOTA-PSMA-03 can be used in diagnostic studies of neuroendocrine differentiated prostate cancer.
    JR11-PEG3-DOTA-PSMA-03
  • 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-125382
    L-797591
    		Agonist
    L-797591 is a selective sst1 agonist. L-797591 mimicks the effects of SRIF-14 and SRIF-28 by potently inhibiting either Forskolin (HY-15371)-stimulated or CRH-stimulated cAMP accumulation.
    L-797591
  • 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-108497R
    L-803087 (Standard)
    		Agonist
    L-803087 (Standard) is the analytical standard of L-803087 (HY-108497). This product is intended for research and analytical applications. L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.
    L-803087 (Standard)
  • 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
    Mazisotine (CNTX-0290) tartrate is an orally active, non-opioid somatostatin receptor 4 (SSTR4) agonist with an EC50 of 4.7 nM. Mazisotine tartrate exerts significant analgesic effects in various nociceptive (inflammatory, osteoarthritic) and neuropathic pain models. Mazisotine tartrate can be used for pain research.
    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
  • HY-102037R
    SSTR5 antagonist 1 (Standard)
    		Antagonist
    SSTR5 antagonist 1 (Standard) is the analytical standard of SSTR5 antagonist 1 (HY-102037). This product is intended for research and analytical applications. SSTR5 antagonist 1 (compound 25a) is a selective and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively.
    SSTR5 antagonist 1 (Standard)
  • HY-P0036S
    Octreotide-d8 TFA
    Octreotide-d8 (SMS 201-995-d8) TFA is the deuterium labeled Octreotide TFA. 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> TFA
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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