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

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16381
    Pasireotide
    Agonist
    Pasireotide (SOM230), 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 can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity.
    Pasireotide
  • 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-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-142701
    SSTR4 agonist 4
    SSTR4 agonist 4 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 4 has the potential for the research of pain (extracted from patent WO2021233428A1, compound 14).
    SSTR4 agonist 4
  • HY-125382
    L-797591
    Agonist
    L-797591 is a selective somatostatin receptor subtype 1 (SSTR1) agonist.
    L-797591
  • HY-P1203A
    BIM-23056 TFA
    Antagonist
    BIM 23056 TFA, a linear octapeptide, is a potent sst3 and sst5 somatostatin receptor antagonist with Ki values of 10.8, 5.7, respectively.
    BIM-23056 TFA
  • HY-106103A
    Seglitide acetate
    Agonist
    Seglitide acetate (MK 678; L 36358 acetate) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide acetate has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide acetate can be used for research on diabetes.
    Seglitide acetate
  • HY-P4992
    Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11)
    Agonist
    Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11) is a somatostatin agonist that can be used in cancer research.
    Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11)
  • HY-P3124
    BIM-23190
    Agonist
    BIM-23190, a somatostatin analog, a selective SSTR2 and SSTR5 agonist, exhibits Ki values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly.
    BIM-23190
  • HY-P0036B
    Octreotide pamoate
    Agonist
    Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.
    Octreotide pamoate
  • HY-110161
    sst2 Receptor agonist-1
    Agonist
    sst2 Receptor agonist-1 is a potent somatostatin receptor subtype 2 (sst2) agonist with a Ki value of 0.025 nM and a cAMP IC50 value of 4.8 nM. sst2 Receptor agonist-1 can inhibit rat growth hormone (GH) secretion and ocular neovascular lesion formation. Antiangiogenic effect.
    sst2 Receptor agonist-1
  • HY-P1201A
    Cyclosomatostatin TFA
    Antagonist
    Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
    Cyclosomatostatin TFA
  • HY-106103
    Seglitide
    Agonist
    Seglitide (MK-678) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide can be used for research on diabetes.
    Seglitide
  • HY-105172A
    TT-232 TFA
    Agonist
    TT-232 TFA (CAP-232 TFA) is an analogue of somatostatin. TT-232 TFA can induce apoptosis of pancreatic tumor cell lines, inhibit tyrosine kinase activity and stimulate tyrosine phosphatase activity in colon tumor cell lines. TT-232 TFA inhibits the proliferation of tumor cells, induces apoptosis of tumor cells and shows strong anti-tumor effects. TT-232 TFA can be used in the development of anti-tumor drugs and the study of apoptosis mechanism.
    TT-232 TFA
  • HY-P10137
    Satoreotide
    Antagonist
    Satoreotide (JR11) is a SSTR2 antagonist. Satoreotide is usually conjugated with radiolabeled chelators used in neuroendocrine tumor imaing.
    Satoreotide
  • HY-108499
    NNC 26-9100
    Agonist
    NNC 26-9100 is a selective somatostatin sst4 receptor full agonist (Ki: 6 nM, EC50: 2 nM). NNC 26-9100 decreases total soluble Aβ42, increases brain neprilysin activity and improves learning.
    NNC 26-9100
  • HY-142699
    SSTR4 agonist 2
    SSTR4 agonist 2 is a potent agonist of somatostatin receptor subtype 4 (SSTR4). SSTR4 pathway inhibits nociceptive and inflammatory processes. SSTR4 agonist 2 has the potential for the research of medical disorders related to SSTR4 (extracted from patent WO2014184275A1, compound 107).
    SSTR4 agonist 2
  • HY-P2229
    Ilatreotide
    Ilatreotide (SDZ CO61), glycated somatostatin derivative, is a highly potent glycated analog of somatostatin with improved oral activity. Ilatreotide can suppress the fasting level and postprandial release of several gastrointestinal and pancreatic hormones. Ilatreotide can be used for the research of gastroenteropancreatic tumors.
    Ilatreotide
Cat. No. Product Name / Synonyms Application Reactivity