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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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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V85758 | Satoreotide (JR11) | 1801415-23-5 | |
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V86783 | Seglitide | 81377-02-8 | Seglitide (MK-678) is an orally active, potent somatostatin receptor 2 (SSTR2) agonist and a competitive SSTR14, SSTR25, and SSTR28 antagonist. |
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V110982 | SSTR4 agonist 6 | 2744188-17-6 | SSTR4 agonist 6 (compound 1) is an SSTR4 agonist. |
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V103243 | SSTR4 agonist-1 | 1638588-92-7 | SSTR4 agonist-1 (Compound 47) is a selective agonist of somatostatin receptor 4 (SSTR4) with EC50 of 4.7 nM. |
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V94958 | SSTR4 agonist-1 tartrate | 2919211-45-1 | SSTR4 agonist-1 tartrate (Formulation 4) is a SSTR4 agonist. |
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V76479 | SSTR5 antagonist 2 hydrochloride | 2988224-31-1 | 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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V85872 | SSTR5 antagonist 3 | 2851454-42-5 | |
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V85399 | SSTR5 antagonist 6 | 1007836-12-5 | |
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V86784 | Tau conotoxin CnVA | 1436463-45-4 | Tau conotoxin CnVA is a small peptide found in the venom of Conus consors pit viper, belonging to the T1 pit viper peptide superfamily. |
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V86780 | Veldoreotide TFA | 2126831-23-8 | Veldoreotide (DG3173) TFA is a somatostatin analog that binds and activates somatostatin receptors (SSTR) 2/4/5. |
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V50990 | WAY-299510 | 1007998-55-1 | STAT3 inhibitor |
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V86786 | Zavolosotine | 2604416-66-0 | Zavolosotine (Compound 1) is an orally active somatostatin receptor type 5 (SST5) agonist with an EC50 of <1 nM. |
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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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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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