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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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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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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V29289 | Octreotide acetate | 79517-01-4 | Octreotide acetate (SMS201-995; Sandostatin, SMS201995; Samilstin; Sandostatina; Octreotide-LAR; Longastatin), the acetate salt of Octreotide, is an octapeptide and somatostatin analogue acting as an agonist for sst2, sst3 and sst5 somatostatin receptors. |
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V70051 | Paltusotine (CRN00808) | 2172870-89-0 | Paltusotine (CRN00808) is an orally bioactive, non-peptide selective somatostatin type 2 (SST2) receptor agonist. |
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V11676 | Pasireotide (SOM-230) | 396091-73-9 | Pasireotide (SOM230; Signifor) isa cyclohexapeptide-based somatostatin mimic approvedfor the treatment of Cushing's disease. |
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V76656 | Pasireotide ditrifluoroacetate (Pasireotide ditrifluoroacetate; SOM230 ditrifluoroacetate; Pasireotide TFA salt) | Pasireotide (SOM230) ditrifluoroacetate is a long-acting cyclohexanide somatostatin analogue that can increase the agonist activity of somatostatin receptors, with pKi of 8.2/9.0 for sst1/2/3/4/5 respectively. | |
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V51075 | PRL-2915 | 209006-18-8 | PRL 2915 is a potent human somatostatin subtype 2 receptor blocker (antagonist) (hsst2) with Ki of 12 nM. |
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V76479 | SSTR5 antagonist 2 hydrochloride | SSTR5 antagonist 2 HCl (compound 10) is a potent, orally bioactive, selective antagonist of growth hormone-suppressing hormone (receptor) subtype 5 (SSTR5) with potential for use in type 2 diabetes. | |
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V50990 | WAY-299510 | 1007998-55-1 | STAT3 inhibitor |
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