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

Somatostatin Receptor

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 Related Products (26):

Cat. No. Product Name Effect Purity
  • HY-17365
    Octreotide acetate Agonist 99.83%
    Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.
  • HY-P0036
    Octreotide Agonist 98.84%
    Octreotide is a somatostatin analog that binds to the somatostatin receptor, mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production.
  • HY-79135
    Pasireotide ditrifluoroacetate
    Pasireotide (ditrifluoroacetate) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively).
  • HY-13466
    MK-4256 Antagonist 99.48%
    MK-4256 is a potent and selective SSTR3 antagonist with IC50s of 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively.
  • HY-P1202A
    CYN 154806 TFA Antagonist 99.97%
    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.
  • HY-111615A
    J-2156 TFA Agonist 99.98%
    J-2156 TFA 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 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.
  • HY-P1206
    CH 275 Agonist
    CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM. CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively. CH 275 can be used for the research of alzheimer’s disease.
  • HY-P3124A
    BIM-23190 hydrochloride Agonist 98.62%
    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.
  • HY-102037
    SSTR5 antagonist 1 Antagonist 99.69%
    SSTR5 antagonist 1 is a potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively. (Compound 25a)
  • HY-79136
    Pasireotide L-aspartate salt 99.44%
    Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).
  • HY-P1932A
    Cortistatin-14 TFA 99.88%
    Cortistatin-14 (TFA), a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 (TFA) shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties.
  • HY-108497
    L-803087 Agonist ≥98.0%
    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.
  • HY-16381
    Pasireotide
    Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).
  • HY-114191
    SSTR5 antagonist 2 Antagonist
    SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM).
  • HY-114191A
    SSTR5 antagonist 2 TFA Antagonist
    SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM).
  • HY-P2545
    [Tyr1]-Somatostatin-14
    [Tyr1]-Somatostatin-14 could binds to SSTR2.
  • HY-P1203A
    BIM-23056 TFA Antagonist
    BIM 23056 TFA, a linear octapeptide, is a potent sst3 and sst5 somatostatin receptor antagonist with Ki values of 10.8, 5.7, respectively.
  • HY-P1932
    Cortistatin-14
    Cortistatin-14, a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties.
  • HY-P3124
    BIM-23190 Agonist
    BIM-23190, a somatostatin analog, a selective SSTR2 and SSTR5 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.
  • HY-P1201A
    Cyclosomatostatin TFA Antagonist
    Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
Isoform Specific Products

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