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-133025
    FK962
    		Activator 99.89%
    FK962 is an enhancer of somatostatin release, exerts cognitive-enhancing actions. Anti-dementia properties.
    FK962
  • HY-108501
    (1R,1'S,3'R/1R,1'R,3'S)-L-054,264
    		Agonist
    (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. (1R,1'S,3'R/1R,1'R,3'S)-L-054,264 can be used in the study of retinal neuromodulation.
    (1R,1'S,3'R/1R,1'R,3'S)-L-054,264
  • HY-P3958
    BIM-23027
    		Agonist 99.76%
    BIM-23027 is a selective agonist of sst2 receptor (EC50=0.32 nM), with similar effect to somatostatin (SRIF), a cyclic tetradecapeptide. BIM-23027 stimulates dopamine release, which is mediated by a Glu-dependent mechanism.
    BIM-23027
  • HY-P4469
    PRL 3195
    		Antagonist
    PRL 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).
    PRL 3195
  • HY-123335
    L-796778
    		Agonist 98.00%
    L-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.
    L-796778
  • HY-P10239
    Tyr3-Octreotate
    		Ligand 99.76%
    Tyr3-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.
    Tyr3-Octreotate
  • HY-177493
    SSTR3 Agonist-1
    		Agonist
    SSTR3 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.
    SSTR3 Agonist-1
  • HY-P1207
    BIM 23052
    		Agonist 99.76%
    BIM 23052 is a somatostatin receptor 5 agonist. BIM 23052 can induce gastric emptying.
    BIM 23052
  • HY-114191
    SSTR5 antagonist 2
    		Antagonist
    SSTR5 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).
    SSTR5 antagonist 2
  • HY-114191A
    SSTR5 antagonist 2 TFA
    		Antagonist
    SSTR5 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).
    SSTR5 antagonist 2 TFA
  • HY-P1959B
    Lanreotide diTFA
    Lanreotide (BIM 23014) diTFA is a somatostatin analogue with antineoplastic activity. Lanreotide diTFA can be used for the research of carcinoid syndrome.
    Lanreotide diTFA
  • HY-P2545
    [Tyr1]-Somatostatin-14
    [Tyr1]-Somatostatin-14 could binds to SSTR2.
    [Tyr1]-Somatostatin-14
  • HY-P4555
    (D-Phe5,Cys6,11,N-Me-D-Trp8)-Somatostatin-14 (5-12) amide
    		Agonist
    (D-Phe5,Cys6,11,N-Me-D-Trp8)-Somatostatin-14 (5-12) amide (Compound 4) is a somatostatin analog with Kds of 0.61, 11.05, 23.5, 1200 and >1000 nM for SSTR5, SSTR3, SSTR2, SSTR1 and SSTR4, respectively.
    (D-Phe5,Cys6,11,N-Me-D-Trp8)-Somatostatin-14 (5-12) amide
  • HY-137273A
    Sucrose octasulfate
    		Activator
    Sucrose octasulfate, a derivative of sulfated oligosaccharides, is a matrix metalloproteinase (MMP) inhibitor. Sucrose octasulfate stimulates the release of somatostatin-like immunoreactivity (SLI) from the stomach by acting directly on D cells in the gastric mucosa. Sucrose octasulfate exerts its ulcer-healing effect by releasing endogenous gastric somatostatin. Sucrose octasulfate can be used as a pharmaceutical excipient and significantly improves wound closure in diabetic foot ulcers caused by nerve ischemia and venous leg ulcers. Sucrose octasulfate can be used in the study of chronic wound healing.
    Sucrose octasulfate
  • HY-123460
    BN-81674
    		Antagonist
    BN-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.
    BN-81674
  • HY-P3901
    [Leu8,D-Trp22,Tyr25] Somatostatin-28
    [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.
    [Leu8,D-Trp22,Tyr25] Somatostatin-28
  • HY-P0042
    BIM-23197
    		Agonist
    BIM-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.
    BIM-23197
  • HY-160156
    SSTR5 antagonist 4
    		Antagonist
    SSTR5 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.
    SSTR5 antagonist 4
  • HY-P0036A
    Octreotide dihydrochloride
    		Agonist
    Octreotide (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.
    Octreotide dihydrochloride
  • HY-142701
    SSTR4 agonist 4
    		Activator
    SSTR4 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.
    SSTR4 agonist 4
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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