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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-105172
    TT-232
    		Agonist 98.96%
    TT-232 (CAP-232), a somatostatin derivative, is a peptide SSTR1/SSTR4 agonist. TT-232 inhibits cancer cell proliferation and induces apoptosis. TT-232 is also a broad-spectrum anti-inflammatory and analgesic agent.
    TT-232
  • HY-P1206
    CH 275
    		Agonist 99.71%
    CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM. CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively. CH 275 can be used for the research of alzheimer’s disease.
    CH 275
  • HY-P4452
    PRL 2915
    		Antagonist 99.57%
    PRL 2915 is a potent human somatostatin subtype 2 receptor (hsst2) antagonist with a Ki of 12 nM.
    PRL 2915
  • HY-79136
    Pasireotide L-aspartate salt
    		Agonist ≥98.0%
    Pasireotide (SOM230) L-aspartate salt, 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 L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity.
    Pasireotide L-aspartate salt
  • HY-P3618
    Cortistatin 29
    		99.22%
    Cortistatin 29 is a neuropeptide. Cortistatin 29 alleviates neuropathic pain. Cortistatin 29 binds with high affinity all somatostatin (SS) receptor subtypes and shows IC50 values of 2.8, 7.1, 0.2, 3.0, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin 29 shows anti-fibrotic effects.
    Cortistatin 29
  • HY-P3124A
    BIM-23190 hydrochloride
    		Agonist 99.64%
    BIM-23190 hydrochloride, a somatostatin analog, a selective SSRT2 and SSRT5 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 hydrochloride
  • HY-P5126
    DOTA-LM3
    		Antagonist 98.22%
    DOTA-LM3 is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 and 68 Ga-DOTA-LM3. 68 Ga-DOTA-LM3 shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis.
    DOTA-LM3
  • HY-108497
    L-803087
    		Agonist ≥98.0%
    L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.
    L-803087
  • HY-P2090A
    Angiopeptin TFA
    		Agonist 99.71%
    Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research.
    Angiopeptin TFA
  • HY-108498
    L-817818
    		Agonist ≥99.0%
    L-817818 is a potent and subtype-selective agonist of the somatostatin receptor. L-817818 provides a direct approach to defining somatostatin receptor physiological functions
    L-817818
  • HY-P1499
    Somatostatin-28 (1-14)
    		Agonist 99.56%
    Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28.
    Somatostatin-28 (1-14)
  • HY-P5362A
    NODAGA-LM3 TFA
    		Antagonist
    NODAGA-LM3 TFA can be labeled by 68Ga for PET imaging. 68Ga-NODAGA-LM3 TFA is a SSTR2 antagonist, and can be used for imaging of SSTR positive paragangliomas.
    NODAGA-LM3 TFA
  • HY-P1202
    CYN 154806
    		Antagonist 99.76%
    CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
    CYN 154806
  • HY-P5128
    DOTA-JR11
    		Antagonist 98.39%
    DOTA-JR11 is a somatostatin receptor 2 （SSTR2）antagonist. DOTA-JR11 can be labeled by 68Ga, used for paired imaging in neuroendocrine tumors (NETs) research.
    DOTA-JR11
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity