Somatostatin Receptor
SSTRs; SSTR
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
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Somatostatin Receptor Inhibitors
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Somatostatin Receptor Agonists
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Somatostatin Receptor Antagonists
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Somatostatin Receptor Activators
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Somatostatin Receptor Modulators
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Somatostatin Receptor Chemicals
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Somatostatin Receptor Control
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Somatostatin Receptor Ligands
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Somatostatin Receptor Related Products (157)
Related Products (157)
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Antibodies (10)
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Somatostatin Receptor Isoform Comparison
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FK962
0 ImagesFK962 is an enhancer of somatostatin release, exerts cognitive-enhancing actions. Anti-dementia properties.
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SSTR4 agonist 6
0 ImagesCat. No.: HY-W1117589CAS No.: 2744188-17-6
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PRL 3195
0 ImagesCat. No.: HY-P4469CAS No.: 341519-04-8PRL 3195 is a somatostatin receptor antagonist with Kis of 6, 17, 66, 1000 and 1000 nM for human somatostatin receptors (sst5, sst2, sst3, sst1 and sst4, respectively).
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(R)-Verapamil
0 ImagesSynonyms: Dexverapamil(R)-Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil (HY-14275). (R)-Verapamil has a relatively low affinity for L-type calcium channels (Cav1.2) (IC50 > 300 μM), and its IC50 for sodium channels (sodium channel) is 3.19 μM. (R)-Verapamil exhibits SSTR2 agonistic activity, with an EC50 of 1.3 μM. (R)-Verapamil significantly downregulates the expression of TXNIP protein in diabetic mouse models and significantly inhibits β-cell apoptosis (apoptosis), effectively controlling blood sugar. (R)-Verapamil can be used as a PET tracer for the function of P-glycoprotein (P-gp).
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L-796778
0 ImagesCat. No.: HY-123335CAS No.: 217480-25-6L-796778 is an agonist of the hsst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796778 is a partial agonist that inhibits forskolin (HY-15371)-stimulated cAMP production with an IC50 value of 18 nM.
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Tyr3-Octreotate
0 ImagesTyr3-Octreotate is a ligand for somatostatin receptor subtype 2 (sst2), with an IC50 value of 1.3 nM against sst2 when labeled with [111In-DTPA], and an IC50 value of 1.6 nM against sst2 when labeled with [90Y-DOTA]. Radiolabeled Tyr3-Octreotate generates cell-associated radioactivity, and acts as both a tumor growth inhibitor and a tumor cytotoxic agent. When radiolabeled with 177Lu or 90Y, Tyr3-Octreotate serves as a peptide receptor radionuclide therapy (PRRT) analog. Tyr3-Octreotate can be used in studies related to pancreatic tumors.
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SSTR3 Agonist-1
0 ImagesCat. No.: HY-177493CAS No.: 3086695-73-7SSTR3 Agonist-1 (Compound EX 38) is an orally active SSTR3 agonist, with an EC50 of 0.14 nM. SSTR3 Agonist-1 reduces the kidney cystic index. SSTR3 Agonist-1 can be used in the research of autosomal dominant polycystic kidney disease.
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SSTR5 antagonist 2
0 ImagesCat. No.: HY-114191CAS No.: 1254730-81-8SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM).
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SSTR5 antagonist 2 TFA
0 ImagesCat. No.: HY-114191ACAS No.: 1254733-98-6SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM).
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Lanreotide diTFA
0 ImagesCat. No.: HY-P1959BCAS No.: 1024499-83-9Synonyms: BIM 23014 diTFALanreotide (BIM 23014) diTFA is a somatostatin analogue with antineoplastic activity. Lanreotide diTFA can be used for the research of carcinoid syndrome.
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[Tyr1]-Somatostatin-14
![[Tyr1]-Somatostatin-14](https://file.medchemexpress.com/product_pic/hy-p2545.gif "Click to View [Tyr1]-Somatostatin-14 Product Detail")
0 ImagesCat. No.: HY-P2545CAS No.: 59481-23-1[Tyr1]-Somatostatin-14 could binds to SSTR2.
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BN-81674
0 ImagesCat. No.: HY-123460CAS No.: 252278-73-2BN-81674 is a somatostatin analogue and a selective antagonist of the non-peptide human somatostatin sst3 receptor (Ki=0.92 nM). In addition, BN-81674 reversed the inhibition of cyclic AMP accumulation induced by 1 nM somatostatin through the sst3 receptor with an IC50 value of 0.84 nM. BN-81674 can be used in cancer research.
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[Leu8,D-Trp22,Tyr25] Somatostatin-28
![[Leu8,D-Trp22,Tyr25] Somatostatin-28](https://file.medchemexpress.com/product_pic/hy-p3901.gif "Click to View [Leu8,D-Trp22,Tyr25] Somatostatin-28 Product Detail")
0 ImagesCat. No.: HY-P3901CAS No.: 77909-99-0[Leu8,D-Trp22,Tyr25] Somatostatin-28 is the analog of Somatostatin-28. Somatostatin-28 is a intestinal peptide containing somatostatin in its C-terminal portion.
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BIM-23197
0 ImagesCat. No.: HY-P0042CAS No.: 168016-90-8BIM-23197 is a selective SST2 (IC50 = 0.19 nM) agonist. BIM-23197 can effectively stimulate intracellular calcium mobilization in cells expressing SST2. BIM-23197 can be used for research on endocrine related conditions.
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SSTR5 antagonist 4
0 ImagesCat. No.: HY-160156CAS No.: 916338-03-9SSTR5 antagonist 4 (compound 1) is a potent, selective and orally active somatostatin subtype 5 (SSTR5) antagonist (hSSTR5 IC50 = 1.3 nM, mSSTR5 IC50 = 1.0 nM). SSTR5 antagonist 4 shows efficacy in mouse oral glucose tolerance test (OGTT) in high fat diet (HFD)-mice. SSTR5 antagonist 4 can be used for type 2 diabetes research.
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Octreotide dihydrochloride
0 ImagesCat. No.: HY-P0036ACAS No.: 1607842-55-6Synonyms: SMS 201-995 dihydrochlorideOctreotide (SMS 201-995) hydrochloride is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide hydrochloride can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide hydrochloride increases Gi activity and reduces intracellular cAMP production. Octreotide hydrochloride has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.
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SSTR4 agonist 4
0 ImagesCat. No.: HY-142701CAS No.: 2747928-27-2SSTR4 agonist 4 is a somatostatin receptor 4 (SSTR4) agonist. SSTR4 agonist 4 functionally activates SSTR4. SSTR4 agonist 4 has the potential for the research of pain.
