2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Somatostatin Receptor

Somatostatin Receptor

SSTRs; SSTR

Somatostatin Receptor

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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:

Somatostatin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-142928
    MAT2A-IN-1
    		Inhibitor
    MAT2A-IN-1 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally high in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-1 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-1 has the potential for the research of cancer diseases (extracted from patent WO2021139775A1, compound 64).
    MAT2A-IN-1
  • HY-P3294
    Onzigolide
    		Agonist
    Onzigolide (BIM-23A760), a chimeric dopamine-somatostatin compound, shows potent agonist activity at both DA type 2 (D2R) and SST type 2 (SSTR2) receptors.
    Onzigolide
  • HY-142930
    MAT2A-IN-3
    		Inhibitor
    MAT2A-IN-3 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally high in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-3 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-3 has the potential for the research of cancer diseases (extracted from patent WO2019191470A1, compound 265).
    MAT2A-IN-3
  • HY-160176
    SSTR5 antagonist 6
    		Antagonist
    SSTR5 antagonist 6 is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with an IC50 of 24 nM. SSTR5 antagonist 6 can be used in the study of type 2 diabetes.
    SSTR5 antagonist 6
  • HY-177278
    SST1 receptor antagonist-1
    		Antagonist
    SST1 receptor antagonist-1 (Compound 23) is a selective Somatostatin receptor 1 (SST1) antagonist with pKds of 9.11 and 8.79 for rSST1 and hSST1, respectively. SST1 receptor antagonist-1 can be used for retinal and endocrine dysfunctions, cancer and neuropsychiatric disorders research.
    SST1 receptor antagonist-1
  • HY-12819
    MK-1421
    		Antagonist
    MK-1421 is a potent and selective sstr3 antagonist. MK-1421 regulates insulin secretion by binding to the sstr3. MK-1421 can be used in the research of type 2 diabetes.
    MK-1421
  • HY-P3903
    [D-Trp8,Tyr11] Somatostatin
    [D-Trp8,Tyr11] Somatostatin is an analogue of somatostatin. Somatostatin is a hormone that regulates a variety of bodily functions. DTrp8 residue can increase stability.
    [D-Trp8,Tyr11] Somatostatin
  • HY-P3897
    [Tyr12] Somatostatin 28 (1-14)
    [Tyr12] Somatostatin 28 (1-14) is an analogue of Somatostatin-28 (1-14) (HY-P1499). Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28.
    [Tyr12] Somatostatin 28 (1-14)
  • HY-142700
    SSTR4 agonist 3
    SSTR4 agonist 3 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 3 has the potential for the research of pain (extracted from patent WO2021233427A1, compound 14).
    SSTR4 agonist 3
  • HY-P3902
    [D-Trp8] Somatostatin-14
    [D-Trp8] Somatostatin-14, a tetradecapeptide, is an analog of Somatostatin more potent than the native Somatostatin.
    [D-Trp8] Somatostatin-14
  • HY-114133
    Depreotide
    		Ligand
    Depreotide is a nove tumor tarcer, can be complexed with technetium-99m (99mTc-depreotide) for optimal imaging properties. 99mTc-depreotide somatostain receptor imaging has been playing an important role in medical diagnosis research. Depreotide can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    Depreotide
  • HY-177493A
    SSTR3 agonist-1 TFA
    		Agonist
    SSTR3 agonist-1 TFA is a potent, orally active, and selective SSTR3 agnoist (EC50 =0.14 nM). SSTR3 agonist-1 TFA binds to SSTR3 receptor to inhibit cAMP activity. SSTR3 agonist-1 TFA decreases kidney weight and kidney cystic index (KCI) in a mouse model of autosomal dominant polycystic kidney disease (ADPKD). SSTR3 agonist-1 TFA can be used for ADPKD research.
    SSTR3 agonist-1 TFA
  • HY-P4957
    Octreotide dimer (parallel)
    		Agonist
    Octreotide dimer parallel is a dimer parallel of Octreotide. Octreotide (HY-P0036) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue.
    Octreotide dimer (parallel)
  • HY-175053
    Pasireotide (aspartate) TFA
    		Agonist
    Pasireotide (aspartate) TFA, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide (aspartate) TFA can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide (aspartate) TFA also exhibits antisecretory, antiproliferative, and proapoptotic activity.
    Pasireotide (aspartate) TFA
  • HY-P2434
    AP102
    AP102 is a dual SSTR2/SSTR5-specific somatostatin analog (SSA). AP102 is a disulfide-bridged octapeptide SSA containing synthetic iodinated amino acids. AP102 binds with subnanomolar affinity to SSTR2 and SSTR5 (IC50: 0.63 and 0.65 nM, respectively). AP102 does not bind to SSTR1 or SSTR3. AP102 can be used for acromegaly and neuroendocrine tumors research.
    AP102
  • HY-RS13832
    SSTR5 Human Pre-designed siRNA Set A
    		Inhibitor

    SSTR5 Human Pre-designed siRNA Set A contains three designed siRNAs for SSTR5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SSTR5 Human Pre-designed siRNA Set A
  • HY-P4100
    Cyclic SSTR agonist octreotide
    		Agonist
    Cyclic SSTR agonist octreotide is a Octreotide (HY-P0036), serving as the cyclic Somatostatin Receptor SSTR agonist.
    Cyclic SSTR agonist octreotide
  • HY-Z15823
    (R)-Verapamil
    		Agonist
    (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).
    (R)-Verapamil
  • HY-108497A
    L-803087 TFA
    		Agonist
    L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.
    L-803087 TFA
  • HY-P0036D
    NOTA-Octreotide
    		Antagonist
    NOTA‑Octreotide is a selective SSTR2‑targeting PET tracer. NOTA‑Octreotide binds specifically to SSTR2 and accumulates in SSTR2‑expressing tissues. NOTA‑Octreotide enables effective imaging of somatostatin receptor‑positive tumors in mice and shows high specific uptake in SSTR2‑expressing organs in healthy rats. NOTA-Octreotide can be used for PET imaging investigation of neuroendocrine tumors..
    NOTA-Octreotide
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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