Somatostatin receptors (SSTR1, 2A and B, 3, 4 and 5) belong to the G protein coupled receptor family. Many human tumors, including the majority of neuroendocrine tumors, breast tumors, some brain tumors, renal cell tumors, lymphomas, and prostate cancer, express somatostatin receptors. By binding to somatostatin receptors, somatostatin produces cytotoxic and cytostatic effects as well as a general secretion-inhibiting effect.
While SSTR5 is selective for somatostatin-28, SSTRs 1-4 exhibit weak selectivity for somatostatin-14 binding. SSTRs 2, 3, and 5 belong to a similar somatostatin receptor subclass based on structural similarity and reactivity for octapeptide and hexapeptide somatostatin receptor analogs; SSTRs 1-4 react poorly with these analogs and belong to a different subclass. Through pertussis toxin-sensitive guanosine triphosphate (GTP)-binding proteins, the inhibition of adenylyl cyclase is functionally linked to all five somatostatin receptors. The mRNA for SSTRs 1–5 is widely expressed in the brain and other peripheral organs, and it shows an overlapping, distinctive pattern that is species- and tissue-specific as well as subtype-specific. SSTR2 and SSTR5 are expressed by all subsets of pituitary cells, with SSTR5 being more prevalent. Pituitary cells coexpress various subtypes of somatostatin receptors.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V70047 | CYN 154806 TFA | 2828432-46-6 | CYN 154806 TFA is a cyclic octapeptide and a potent and specific antagonist of somatostatin sst2 receptor. |
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V111183 | Des-threoninol-octreotide | 160841-00-9 | Dethreonol octreotide (compound 13) is a somatostatin analog. |
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V70055 | DOTA-JR11 | 1039726-31-2 | DOTA-JR11 is an antagonist of the somatostatin receptor SSTR2. |
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V70049 | DOTA-LM3 | 1192362-32-5 | DOTA-LM3 is a somatostatin receptor (SSTR) antagonist. |
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V77072 | DOTA-LM3 TFA | DOTA-LM3 TFA is a somatostatin receptor (SSTR) antagonist. | |
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V70050 | J-2156 TFA | 2387505-73-7 | J-2156 TFA is a potent and specific somatostatin receptor type 4 (SST4) agonist/activator with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. |
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V108979 | JR11-PEG3-DOTA-PSMA-03 | JR11-PEG3-DOTA-PSMA-03 (compound 2) is an RDC-related compound containing the chelating agent DOTA, the JR11 peptide (SSTR2 antagonist), and the PSMA ligand. | |
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V108937 | JR11-PEG3-HBED-CC-PSMA-03 | JR11-PEG3-HBED-CC-PSMA-03 (Compound 1) is an RDC-related compound containing the chelating agent HBED-CC, the JR11 peptide (SSTR2 antagonist), and the PSMA ligand. | |
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V50904 | L-779976 | 214770-19-1 | somatostatin receptor agonist |
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V138571 | L-796778 acetate | 2922280-21-3 | L-796778 acetate is a selective agonist of the sst3 receptor. |
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V138572 | L-797591 hydrochloride | 3026641-74-4 | L-797591 hydrochloride is a selective sst1 agonist. |
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V70056 | L-803087 TFA | 1786412-46-1 | L-803087 TFA is a potent and specific somatostatin sst4 receptor agonist/activator with a Ki of 0.7 nM and is more than 280 times more selective for sst4 than other somatostatin receptors. |
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V120202 | L803 | 348089-28-1 | L803 is a selective somatostatin receptor type 4 (SST4) agonist. |
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V4290 | MK-4256 | 1104599-69-0 | JNJ-46778212 (also known as VU 0409551) is a novel, potent, orally bioavailable metabotropic glutamate receptor subtype 5 (mGlu5) positive allosteric modulator (PAMs) with an EC50 of 260 nM. |
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V86785 | MMC(TMZ)-TOC | MMC(TMZ)-TOC has high binding affinity and selectivity for somatostatin receptor subtype 2 (SSTR2). | |
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V103894 | MMC(TMZ)-TOC TFA | MMC(TMZ)-TOC TFA has high binding affinity and selectivity for somatostatin receptor subtype 2 (SSTR2). | |
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V51088 | Nendratareotide | 2251119-65-8 | Nendratareotide is a somatostatin analog. |
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V70060 | NODAGA-LM3 | 1415238-78-6 | NODAGA-LM3 can be labeled with 68Ga and used for PET imaging. |
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V80964 | NODAGA-LM3 TFA | NODAGA-LM3 TFA can be labeled with 68Ga and used for PET imaging. | |
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V141580 | NOTA-Octreotide | 1427427-01-7 | NOTA-Octreotide is a PET tracer that selectively targets SSTR2. |
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