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-79135
    Pasireotide ditrifluoroacetate
    		Agonist 99.56%
    Pasireotide (SOM230) ditrifluoroacetate, 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 ditrifluoroacetate exhibits antisecretory, antiproliferative, and proapoptotic activity.
    Pasireotide ditrifluoroacetate
  • HY-P1202A
    CYN 154806 TFA
    		Antagonist 99.81%
    CYN 154806 TFA, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
    CYN 154806 TFA
  • HY-P4452
    PRL 2915
    		Antagonist 99.92%
    PRL 2915 is a potent human somatostatin subtype 2 receptor (hsst2) antagonist with a Ki of 12 nM.
    PRL 2915
  • HY-P5362
    NODAGA-LM3
    		Antagonist 99.33%
    NODAGA-LM3 can be labeled by 68Ga for PET imaging. 68Ga-NODAGA-LM3 is a SSTR2 antagonist, and can be used for imaging of SSTR positive paragangliomas. NODAGA-LM3 can be labeled with [68Ga] for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    NODAGA-LM3
  • HY-P10137
    Satoreotide
    		Antagonist 98.88%
    Satoreotide (JR11) is a SSTR2 antagonist. Satoreotide is usually conjugated with radiolabeled chelators used in neuroendocrine tumor imaing.
    Satoreotide
  • HY-P5011
    Cortistatin-17 (human)
    		Modulator 99.04%
    Cortistatin-17 (human) is a somatostatin neuropeptide with potential for studying diseases such as cancer, inflammation, autoimmunity, fibrosis, and pain.
    Cortistatin-17 (human)
  • HY-P1203
    BIM-23056
    		Antagonist 99.98%
    BIM 23056, a linear octapeptide, is a potent sst3 and sst5 somatostatin receptor antagonist with Ki values of 10.8, 5.7, respectively.
    BIM-23056
  • HY-P1212
    Cortistatin 14 (mouse, rat)
    		99.96%
    Cortistatin 14, mouse, rat (CST-14, human, rat), a neuropeptide with neuronal depressant and sleep modulating properties, can bind to all five cloned somatostatin receptors (SSTRs) and ghrelin receptor to exert its biological activities and co-exists with GABA within the cortex and hippocampus.
    Cortistatin 14 (mouse, rat)
  • HY-P3124A
    BIM-23190 hydrochloride
    		Agonist 99.33%
    BIM-23190 hydrochloride, a somatostatin analog, a selective SSRT2 and SSRT5 agonist, exhibits Ki values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly.
    BIM-23190 hydrochloride
  • HY-P0024A
    Veldoreotide TFA
    		Agonist 98.97%
    Veldoreotide (DG3173) TFA a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide TFA inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent
    Veldoreotide TFA
  • HY-139347
    Mazisotine
    		Agonist 99.54%
    SSTR4 agonist-1 (Compound 47) is a selective agonist for somatostatin receptor subtype 4 (SSTR4) with an EC50 of 4.7 nM. SSTR4 agonist-1 reveals a half-life > 130 minutes in human liver microsomes.
    Mazisotine
  • HY-114191B
    SSTR5 antagonist 2 hydrochloride
    		Antagonist 98.85%
    SSTR5 antagonist 2 hydrochloride is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of type 2 diabetes mellitus (T2DM).
    SSTR5 antagonist 2 hydrochloride
  • HY-108497
    L-803087
    		Agonist 99.66%
    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
  • HY-P1499
    Somatostatin-28 (1-14)
    		Agonist 99.75%
    Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28.
    Somatostatin-28 (1-14)
  • HY-79136
    Pasireotide L-aspartate salt
    		Agonist ≥98.0%
    Pasireotide (SOM230) L-aspartate salt, 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 L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity.
    Pasireotide L-aspartate salt
  • HY-P2090A
    Angiopeptin TFA
    		Agonist 99.01%
    Angiopeptin TFA, 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 TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research.
    Angiopeptin TFA
  • HY-123335A
    L-796778 acetate
    		Agonist 98.00%
    L-796778 acetate is a selective agonist of the sst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796778 acetate is a partial agonist that inhibits Forskolin (HY-15371)-stimulated cAMP production with an IC50 value of 18 nM. L-796778 acetate has anticonvulsant effect.
    L-796778 acetate
  • HY-123499
    SRA880
    		Antagonist 98.22%
    SRA880 is a non-peptide and selective somatostatin sst(1) receptor antagonist. SRA880 exhibits antidepressant-like effects when in combination with Imipramine (HY-B1490A) .
    SRA880
  • HY-106103A
    Seglitide acetate
    		Agonist 99.30%
    Seglitide acetate (MK 678; L 36358 acetate) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide acetate has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide acetate can be used for research on diabetes.
    Seglitide acetate
  • HY-P1373
    Neuronostatin-13 (human)
    		98.72%
    Neuronostatin-13 human is a 13-amino acid peptide hormone encoded by the somatostatin gene and plays an important role in the regulation of hormonal and cardiac function.
    Neuronostatin-13 (human)
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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