2. Signalwege
  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
Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • HY-P10137
    Satoreotide
    		Antagonist 98.80%
    Satoreotide (JR11) is a somatostatin receptor subtype 2 (sstr2)-selective antagonist. Satoreotide can be used as a PET imaging agent when labeled with 68Ga. Satoreotide can be used for cancer research.
    Satoreotide
  • HY-P1201
    Cyclosomatostatin
    		Antagonist 99.56%
    Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
    Cyclosomatostatin
  • HY-105172
    TT-232
    		Agonist 98.72%
    TT-232 (CAP-232), a somatostatin derivative, is a peptide SSTR1/SSTR4 agonist. TT-232 inhibits cancer cell proliferation and induces apoptosis. TT-232 is also a broad-spectrum anti-inflammatory and analgesic agent.
    TT-232
  • HY-P5362
    NODAGA-LM3
    		Antagonist 99.65%
    NODAGA-LM3 is a ligand that can cross the blood-brain barrier and targets somatostatin receptor SSTR2 with high affinity (IC50 = 1.3 nM). NODAGA-LM3 does not trigger the internalization of SSTR2 and can inhibit agonist-induced internalization processes. NODAGA-LM3 shows low uptake in normal tissues such as the liver and spleen, but high uptake in the lungs and blood pool. 68Ga-labeled NODAGA-LM3 can serve as a PET imaging agent for well-differentiated neuroendocrine tumors, and is applied in studies related to small cell lung cancer and well-differentiated neuroendocrine tumors.
    NODAGA-LM3
  • 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-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 98.30%
    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-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-111615
    J-2156
    		Agonist 99.88%
    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-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-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-P1959
    Lanreotide
    		Activator 98.86%
    Lanreotide (BIM 23014) is a somatostatin analogue with antineoplastic activity. Lanreotide can be used for the research of carcinoid syndrome.
    Lanreotide
  • HY-P1373
    Neuronostatin-13 (human)
    		99.53%
    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)
  • HY-P2112
    DOTA-NOC
    		99.22%
    DOTA-NOC (DOTA-Nal3-octreotide) is a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5. DOTA-NOC can be used for labeling with various radiometals, and development of radiopeptide imaging. DOTA-NOC can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA-NOC
  • 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-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-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-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-106103A
    Seglitide acetate
    		Agonist 98.76%
    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-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)
Art. -Nr. Produktname / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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