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 99.96%
    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
    		99.98%
    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 99.93%
    Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.
    Octreotide acetate
  • HY-16381
    Pasireotide
    		Agonist 99.94%
    Pasireotide (SOM230), 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 can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity.
    Pasireotide
  • HY-P1959A
    Lanreotide acetate
    		99.84%
    Lanreotide (BIM 23014) acetate is a somatostatin analogue with antineoplastic activity. Lanreotide acetate can be used for the research of carcinoid syndrome.
    Lanreotide acetate
  • HY-P11655
    NOTA-TATE
    		Ligand
    NOTA-TATE is a somatostatin receptor 2 (SSTR2) binder. NOTA-TATE binds to SSTR2 to enable targeting of SSTR2-positive tumour cells for PET imaging. NOTA-TATE can be used for the research of neuroendocrine tumours.
    NOTA-TATE
  • HY-125382A
    L-797591 hydrochloride
    		Agonist 99.81%
    L-797591 hydrochloride is a selective sst1 agonist. L-797591 hydrochloride mimicks the effects of SRIF-14 and SRIF-28 by potently inhibiting either Forskolin (HY-15371)-stimulated or CRH-stimulated cAMP accumulation.
    L-797591 hydrochloride
  • HY-W1117589
    SSTR4 agonist 6
    		Agonist
    SSTR4 agonist 6 (Compound 1) is a SSTR4 agonist. SSTR4 agonist 6 can be used for pain research.
    SSTR4 agonist 6
  • HY-P1202
    CYN 154806
    		Antagonist 99.97%
    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-P3954
    Somatostatin-28 (sheep, human rat mouse)
    		Inhibitor 99.67%
    Somatostatin-28 (sheep, human rat mouse) is a biologically active polypeptide, synthesised in the proximal intestinal epithelial cells. Somatostatin-28 (sheep, human rat mouse) suppresses glucose-stimulated insulin secretion without affecting circulating basal insulin concentration. Somatostatin-28 (sheep, human rat mouse) also targets to somatostatin receptor subtype 5 (SSTR5) to regulate GLP-1 secretion.
    Somatostatin-28 (sheep, human rat mouse)
  • HY-13466
    MK-4256
    		Antagonist 99.07%
    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-P5126
    DOTA-LM3
    		Antagonist 99.37%
    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 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA-LM3
  • HY-P5128
    DOTA-JR11
    		Antagonist 99.14%
    DOTA-JR11 is a somatostatin receptor 2 （SSTR2）antagonist. DOTA-JR11 can be labeled by 68Ga, used for paired imaging in neuroendocrine tumors (NETs) research. DOTA-JR11 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA-JR11
  • HY-111615A
    J-2156 TFA
    		Agonist 99.88%
    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-16381A
    Pasireotide acetate
    		Agonist 99.92%
    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-P1932A
    Cortistatin-14 TFA
    		99.99%
    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-139347
    Mazisotine
    		Agonist 99.54%
    Mazisotine (CNTX-0290) is an orally active, non-opioid somatostatin receptor 4 (SSTR4) agonist with an EC50 of 4.7 nM. Mazisotine exerts significant analgesic effects in various nociceptive (inflammatory, osteoarthritic) and neuropathic pain models. Mazisotine can be used for pain research.
    Mazisotine
  • HY-102037
    SSTR5 antagonist 1
    		Antagonist 99.91%
    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-P1206
    CH 275
    		Agonist 99.58%
    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.
    CH 275
  • HY-P1212
    Cortistatin 14 (mouse, rat)
    		99.45%
    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)
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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