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-P0036
    Octreotide
    		Agonist 99.64%
    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
  • HY-P1932
    Cortistatin-14
    		99.21%
    Cortistatin-14 is a neuropeptide that shares structural similarities with somatostatin, working by binding to somatostatin receptors (sst1-sst5). Cortistatin-14 (TFA) has anticonvulsant, neuroprotective effects, and significant anti-inflammatory properties.
    Cortistatin-14
  • HY-17365
    Octreotide acetate
    		Agonist 99.97%
    Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.
    Octreotide acetate
  • HY-16381A
    Pasireotide acetate
    		Agonist 99.82%
    Pasireotide (SOM230) acetate, 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 acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity.
    Pasireotide acetate
  • HY-13466
    MK-4256
    		Antagonist 98.01%
    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.
    MK-4256
  • HY-120287
    L-054522
    		Agonist
    L-054522 is an agonist for somatostatin receptor subtype 2 with Kd of 0.01 nM. L-054522 inhibits growth hormone release from rat primary pituitary cell (IC50=0.05 nM) and glucagon and insulin release from isolated mouse pancreatic islet cell (IC50=0.05 nM and 12 nM).
    L-054522
  • HY-P2150
    Cortistatin-29
    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
  • HY-12819
    MK-1421
    		Antagonist
    MK-1421 is a potent and selective sstr3 antagonist. MK-1421 regulates insulin secretion by binding to the sstr3. MK-1421 can be used in the research of type 2 diabetes.
    MK-1421
  • 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-102037
    SSTR5 antagonist 1
    		Antagonist 99.84%
    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
  • HY-109155
    Paltusotine
    		Agonist 99.52%
    Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.Paltusotine can be used in research on acromegaly and neuroendocrine tumors.
    Paltusotine
  • HY-P1201
    Cyclosomatostatin
    		Antagonist 99.52%
    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-145778
    AGI-41998
    		99.94%
    AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-41998 is a brain-penetrant compound. AGI-41998 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease.
    AGI-41998
  • HY-P1932A
    Cortistatin-14 TFA
    		99.85%
    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.
    Cortistatin-14 TFA
  • HY-111615A
    J-2156 TFA
    		Agonist 99.72%
    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.
    J-2156 TFA
  • HY-P1202
    CYN 154806
    		Antagonist 99.76%
    CYN 154806, 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
  • HY-P5126
    DOTA-LM3
    		Antagonist 98.22%
    DOTA-LM3 is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 and 68 Ga-DOTA-LM3. 68 Ga-DOTA-LM3 shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis.
    DOTA-LM3
  • 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-P1203
    BIM-23056
    		Antagonist 99.94%
    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-145777
    AGI-43192
    		99.53%
    AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease.
    AGI-43192
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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