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-P3618
    Cortistatin-29 (reduced)
    		98.12%
    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 (reduced)
  • HY-108498
    L-817818
    		Agonist 99.80%
    L-817818 is a potent and subtype-selective agonist of the somatostatin receptor. L-817818 provides a direct approach to defining somatostatin receptor physiological functions
    L-817818
  • HY-108499
    NNC 26-9100
    		Agonist 99.3%
    NNC 26-9100 is a selective somatostatin sst4 receptor full agonist (Ki: 6 nM, EC50: 2 nM). NNC 26-9100 decreases total soluble Aβ42, increases brain neprilysin activity and improves learning.
    NNC 26-9100
  • 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-P10758
    Alkyne-βAG-TOCA
    		Agonist 98.99%
    Alkyne-βAG-TOCA, an octreotide derivative, targets somatostatin receptor type 2 (SST2). Alkyne-βAG-TOCA can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    Alkyne-βAG-TOCA
  • HY-P5014
    Cortistatin-29 (human)
    		Modulator 98.48%
    Cortistatin-29 (human) is a somatostatin neuropeptide with potential for studying diseases such as cancer, inflammation, autoimmunity, fibrosis, and pain.
    Cortistatin-29 (human)
  • HY-P0024
    Veldoreotide
    		Activator
    Veldoreotide (DG3173) a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide inhibits growth hormone (GH) secretion in adenomas compared withOctreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent
    Veldoreotide
  • HY-142699
    SSTR4 agonist 2
    SSTR4 agonist 2 is a potent agonist of somatostatin receptor subtype 4 (SSTR4). SSTR4 pathway inhibits nociceptive and inflammatory processes. SSTR4 agonist 2 has the potential for the research of medical disorders related to SSTR4 (extracted from patent WO2014184275A1, compound 107).
    SSTR4 agonist 2
  • HY-163317A
    MMC(TMZ)-TOC TFA
    MMC(TMZ)-TOC TFA has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC TFA targets delivery of TMZ to SSTR2-positive tumor cells. MMC(TMZ)-TOC TFA can be used for the research of cancer.
    MMC(TMZ)-TOC TFA
  • HY-P3899A
    [Nle8] Somatostatin (1-28) (TFA)
    		Chemical 99.86%
    [Nle8] Somatostatin (1-28) TFA is a derivative of somatosttin (1-28) with norleucine replacing methionine in position 8. [Nle8] Somatostatin (1-28) TFA increases the amylase release.[Nle8] Somatostatin (1-28) TFA increases the cyclic AMP in pancreatic acini .
    [Nle8] Somatostatin (1-28) (TFA)
  • HY-P5362A
    NODAGA-LM3 TFA
    		Antagonist
    NODAGA-LM3 TFA can be labeled by 68Ga for PET imaging. 68Ga-NODAGA-LM3 TFA is a SSTR2 antagonist, and can be used for imaging of SSTR positive paragangliomas. NODAGA-LM3 TFA can be labeled with [68Ga] for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    NODAGA-LM3 TFA
  • HY-108768
    Pasireotide pamoate
    		Agonist 99.47%
    Pasireotide (SOM230) pamoate, 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 pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.
    Pasireotide pamoate
  • HY-P3899
    [Nle8] Somatostatin (1-28)
    		Chemical
    [Nle8] Somatostatin (1-28) is a derivative of somatosttin (1-28) with norleucine replacing methionine in position 8. [Nle8] Somatostatin (1-28) increases the amylase release.[Nle8] Somatostatin (1-28) increases the cyclic AMP in pancreatic acini .
    [Nle8] Somatostatin (1-28)
  • HY-133025
    FK962
    		Activator 99.89%
    FK962 is an enhancer of somatostatin release, exerts cognitive-enhancing actions. Anti-dementia properties.
    FK962
  • HY-137273
    Sucrose octasulfate sodium
    		Activator 98.0%
    Sucrose octasulfate is a component of sulfoaluminum. Sucrose octasulfate stimulates the release of somatostatin-like immunoreactivity (SLI) from the stomach by acting directly on D cells in the gastric mucosa. Sucrose octasulfate exerts its ulcer-healing effect by releasing endogenous gastric somatostatin Sucrose octasulfate can be used for anti-gastric ulcer research .
    Sucrose octasulfate sodium
  • HY-111615
    J-2156
    		Agonist
    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-P4469
    PRL 3195
    		Antagonist
    PRL 3195 is a somatostatin receptor antagonist with Kis of 6, 17, 66, 1000 and 1000 nM for human somatostatin receptors (sst5, sst2, sst3, sst1 and sst4, respectively).
    PRL 3195
  • HY-123335
    L-796778
    		Agonist 98.00%
    L-796778 is an agonist of the hsst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796778 is a partial agonist that inhibits forskolin (HY-15371)-stimulated cAMP production with an IC50 value of 18 nM.
    L-796778
  • HY-P10741
    DOTA-EB-TATE
    		Activator
    DOTA-EB-TATE is composed of SST peptide derivative, DOTA-octreotate conjugated a common to an Evans blue analog (EB). DOTA-EB-TATE is a peptide drug conjugate (PDC) improves the pharmacokinetics of SSTR2 analogs and reduces PRRT toxicity. DOTA-EB-TATE can also be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA-EB-TATE
  • HY-P10239
    Tyr3-Octreotate
    		99.76%
    Tyr3-Octreotate is a somatostatin analog. Tyr3-Octreotate exhibits high uptake into tumor, that is capable to be labeled with radioactive metal and thus exhibits antitumor efficacy. Tyr3-Octreotate can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    Tyr3-Octreotate
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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