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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V70057 | (1R,1'S,3'R/1R,1'R,3'S)-L-054,264 | 208706-12-1 | (1R,1'S,3'R/1R,1'R,3'S)-L-054,264 is a selective, non-peptide human somatostatin receptor subtype 2 (sst2) agonist. |
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V70058 | [Nle8] Somatostatin (1-28) | 84768-30-9 | [Nle8] Somatostatin (1-28) is an analogue of somatostatin (1-28) with norleucine at position 8 replacing methionine. |
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V70053 | Angiopeptin TFA (Angiopeptin trifluoroacetate) | 2478421-60-0 | Angiopeptin TFA is a cyclic octapeptide analog of somatostatin and a partial agonist of sst2/sst5 receptors with IC50s of 0.26 nM and 6.92 nM respectively. |
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V70052 | BIM-23056 | 150155-61-6 | BIM 23056 is a linear octapeptide that is a potent sst3 and sst5 somatostatin receptor antagonist (inhibitor) with Kis of 10.8 and 5.7, respectively. |
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V70061 | BIM-23056 TFA | 1426173-61-6 | BIM 23056 TFA is a linear octapeptide and a potent sst3 and sst5 somatostatin receptor antagonist (inhibitor) with Kis of 10.8 and 5.7 respectively. |
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V50993 | BIM-23190 | 182153-96-4 | BIM-23190 is an analog of somatostatin and a selective agonist of SSTR2 and SSTR5. |
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V77206 | BIM-23190 hydrochloride | BIM-23190 HCl is an analog of somatostatin and a selective agonist of SSTR2 and SSTR5. | |
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V70054 | CH 275 | 174688-78-9 | CH 275 is a bioactive peptide analog of somatostatin that binds to somatostatin receptor 1 (sst1) (Ki=52 nM). |
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V77140 | Cortistatin 29 | Cortistatin 29 is a neuropeptide. | |
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V70062 | Cortistatin-29 (human) | 1815618-16-6 | Cortistatin-29 (human) is a somatostatin neuropeptide with potential for studying diseases like cancer, inflammation, autoimmunity, fibrosis, and pain. |
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V78951 | Cyclic SSTR agonist octreotide | Cyclic SSTR agonist octreotide is an Octreotide that works as an agonist of the somatostatin receptor (SSTR). | |
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V70048 | Cyclosomatostatin | 84211-54-1 | Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. |
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V78957 | Cyclosomatostatin TFA | Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. | |
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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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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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V50904 | L-779976 | 214770-19-1 | somatostatin receptor 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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