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-114191B
    SSTR5 antagonist 2 hydrochloride
    		Antagonist 98.85%
    SSTR5 antagonist 2 hydrochloride is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of type 2 diabetes mellitus (T2DM).
    SSTR5 antagonist 2 hydrochloride
  • HY-P2090A
    Angiopeptin TFA
    		Agonist 99.01%
    Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research.
    Angiopeptin 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-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-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-P5126A
    DOTA-LM3 TFA
    		Antagonist 98.75%
    DOTA-LM3 TFA 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 TFA is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 TFA and 68 Ga-DOTA-LM3 TFA. 68 Ga-DOTA-LM3 TFA shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 TFA can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis. DOTA-LM3 (TFA) can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA-LM3 TFA
  • HY-137273
    Sucrose octasulfate sodium
    		Activator 98.0%
    Sucrose octasulfate sodium, a derivative of sulfated oligosaccharides, is a matrix metalloproteinase (MMP) inhibitor. Sucrose octasulfate sodium stimulates the release of somatostatin-like immunoreactivity (SLI) from the stomach by acting directly on D cells in the gastric mucosa. Sucrose octasulfate sodium exerts its ulcer-healing effect by releasing endogenous gastric somatostatin. Sucrose octasulfate sodium can be used as a pharmaceutical excipient and significantly improves wound closure in diabetic foot ulcers caused by nerve ischemia and venous leg ulcers. Sucrose octasulfate sodium can be used in the study of chronic wound healing.
    Sucrose octasulfate sodium
  • 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-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-142699
    SSTR4 agonist 2
    		99.39%
    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-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-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-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-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-P3062
    [Tyr11]-Somatostatin
    		99.55%
    [Tyr11]-Somatostatin is a neuroavtive peptide for proteomics research. Somatostatin is one of many neuroactive substances that influence retinal physiology.
    [Tyr11]-Somatostatin
  • HY-106103
    Seglitide
    		Agonist 99.30%
    Seglitide (MK-678) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide can be used for research on diabetes.
    Seglitide
  • 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 is a ligand that can cross the blood-brain barrier and targets somatostatin receptor SSTR2 with high affinity (IC50 = 1.3 nM). NODAGA-LM3 TFA does not trigger the internalization of SSTR2 and can inhibit agonist-induced internalization processes. NODAGA-LM3 TFA 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 TFA 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 TFA
  • 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)
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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