Catalog No.
Product Name
Application
Product Information
Citations
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somatostatin receptor antagonist
Octreotide is a peptide agonist for sst2, sst3 and sst5 somatostatin receptors. IC50/Kd values (nM) at cloned human somatostatin receptors are: 290 - 1140 (sst1), 0.4 - 2.1 (sst2), 4.4 - 34.5 (sst3), > 1000 (sst4), and 5.6 - 32 (sst5).- Ida Vang Andersen, .et al. , Nucl Med Biol, 2024, May-Jun:132-133:108905 PMID: 38555651
- Somatostatin is an endogenous peptide noted to inhibit the release of growth hormone, insulin and glucagon.
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somatostatin receptor 2 antagonist
CYN-154806 is a potent selective somatostatin receptor 2 (sst2) antagonist.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Neuronostatin-13 human is a 13-amino acid peptide hormone encoded by the somatostatin gene and plays an important role in the regulation of hormonal and cardiac function.
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Somatostatin Receptor agonist
Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively). - Octreotide is a somatostatin analog that binds to the somatostatin receptor, mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production.
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SSTR5 antagonist
SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM). -
SST4 receptor agonist
J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg/kg, respectively. -
SSTR5 antagonist
SSTR5 antagonist 1 is a potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively. (Compound 25a). -
Somatostatin receptors agonist
Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively). -
SSTR5 antagonist
SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM). - Cyclic somatostatin (SRIF-14) is a growth hormone-release inhibiting factor used in the research of severe, acute hemorrhages of gastroduodenal ulcers. Cyclic somatostatin is a neuropeptide co-stored with acetylcholine in the cardiac parasympathetic innervation, exerts influences directly on contraction of ventricular cardiomyocytes. Cyclic somatostatin inhibits the contractile response of isoprenaline with an IC50 value of 13 nM. Cyclic somatostatin can be used for the research of cardiovascular disease.
- Cortistatin-14, a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties.
- Pasireotide (SOM230) acetate, 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 acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity.
- Lanreotide (BIM 23014) acetate is a somatostatin analogue with antineoplastic activity. Lanreotide acetate can be used for the research of carcinoid syndrome.
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sst2 receptor antagonist
CYN 154806 TFA, 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. -
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.
- Somatostatin-28 (sheep, human rat mouse) is a biologically active polypeptide, synthesised in the proximal intestinal epithelial cells. Somatostatin-28 (sheep, human rat mouse) suppresses glucose-stimulated insulin secretion without affecting circulating basal insulin concentration. Somatostatin-28 (sheep, human rat mouse) also targets to somatostatin receptor subtype 5 (SSTR5) to regulate GLP-1 secretion.
- 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.
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Somatostatin Receptor Agonist
Octreotide dihydrochloride is a synthetic octapeptide that acts as an agonist for somatostatin receptors, primarily targeting subtypes 2, 3, and 5. By increasing Gi protein activity, it effectively reduces intracellular cAMP levels, contributing to its antitumor effects. Octreotide dihydrochloride is utilized in research applications related to apoptosis and is particularly relevant in studies of acromegaly and other disorders associated with aberrant somatostatin signaling. -
Verapamil Enantiomer
(R)-Verapamil is an enantiomer of the calcium channel blocker Verapamil, primarily acting on sodium channels with an IC50 of 3.19 μM. It exhibits agonistic activity on somatostatin receptor 2 (SSTR2), with an EC50 of 1.3 μM. In preclinical studies, (R)-Verapamil has demonstrated the ability to downregulate TXNIP protein expression and inhibit β-cell apoptosis in diabetic mouse models, contributing to effective blood glucose control. Additionally, it can be utilized as a PET tracer to assess P-glycoprotein function, making it a valuable tool in metabolic and pharmacological research. -
Somatostatin Receptor Agonist
Octreotide pamoate is a synthetic octapeptide and a somatostatin receptor agonist that primarily targets subtypes 2, 3, and 5. It enhances Gi protein activity, leading to a reduction in intracellular cAMP levels. Octreotide pamoate exhibits antitumor activity and induces apoptosis, making it valuable for research in conditions such as acromegaly and other diseases related to somatostatin signaling. Its unique pharmacological profile allows for exploration in various therapeutic applications and biological studies. -
Antitumor Somatostatin Analogue
TT-232 TFA is a somatostatin analogue that primarily targets antitumor activity. It has been shown to effectively induce apoptosis in pancreatic tumor cell lines while simultaneously inhibiting tyrosine kinase activity and stimulating tyrosine phosphatase activity in colon tumor cell lines. TT-232 TFA demonstrates strong anti-tumor effects by inhibiting tumor cell proliferation and promoting apoptosis. This compound is valuable for the development of anti-tumor therapeutics and for investigating the mechanisms of apoptosis. -
SSTR2 Ligand
Edotreotide is a selective ligand for the somatostatin receptor subtype 2 (SSTR2), capable of competitive binding to the receptor. It facilitates the targeted delivery of radionuclides, such as 90Y, 177Lu, and 68Ga, to SSTR-positive tumors, promoting tumor cell apoptosis through the emission of β rays. Edotreotide's strong tumor-targeting capabilities make it a valuable tool in the development of radionuclide-drug conjugates (RDCs) and in research applications focused on neuroendocrine tumors, including metastatic carcinoids and lung and thymus neuroendocrine tumors. -
SSTR2 Antagonist
Satoreotide is a selective antagonist of the somatostatin receptor subtype 2 (SSTR2). It has demonstrated potential in enhancing neuroendocrine tumor imaging when conjugated with radiolabeled chelators. This compound is significant in research applications focused on the development of targeted imaging agents for diagnostic purposes in oncological settings. -
Somatostatin Receptor Ligand
DOTA-NOC (DOTA-Nal3-octreotide) is a high-affinity ligand for somatostatin receptor subtypes 2, 3, and 5. This compound is primarily utilized for radiolabeling with various radiometals, facilitating the development of radiopeptide imaging techniques. Additionally, DOTA-NOC plays a crucial role in the synthesis and research of Radionuclide-Drug Conjugates (RDCs), making it a valuable reagent in oncological and diagnostic studies. -
Peptide Drug Conjugate
DOTA-EB-TATE is a peptide drug conjugate composed of a somatostatin (SST) peptide derivative, DOTA-octreotate, conjugated to an Evans blue analog. This compound enhances the pharmacokinetics of somatostatin receptor subtype 2 (SSTR2) analogs while decreasing associated toxicity in peptide receptor radionuclide therapy (PRRT). DOTA-EB-TATE is also applicable in the synthesis and research of radionuclide-drug conjugates (RDCs), making it valuable for investigations in targeted cancer therapies. -
Tumor Tracer
Pentetreotide is a somatostatin analog conjugated with diethylenetriaminopentaacetic acid (DTPA) and labeled with indium. It serves as a tumor tracer, primarily utilized in nuclear medicine imaging to detect neuroendocrine tumors and their metastases. The compound's ability to bind to somatostatin receptors enables effective scintigraphy, making it a valuable tool in oncological diagnostics and research applications focused on neuroendocrine malignancies. -
Antitumor Agent
Tyr3-Octreotate is a somatostatin analog that specifically targets somatostatin receptors. It demonstrates significant uptake in tumor tissues, allowing for effective labeling with radioactive metals, which enhances its antitumor efficacy. This compound is valuable for the development and research of Radionuclide-Drug Conjugates (RDCs) in cancer therapy. -
Biochemical Assay Reagent
DOTA-Octreotide is a chelator-conjugated peptide targeting somatostatin receptors, primarily used in biochemical assays. It facilitates the research of cancer by enabling the synthesis of radionuclide-drug conjugates (RDCs) when combined with radioactive isotopes. DOTA-Octreotide is crucial for studies in tumor imaging and targeted radiotherapy applications, enhancing the understanding of receptor-targeted approaches in oncology research. -
Tumor Tarcer
Depreotide is a novel tumor targeting agent that selectively binds to somatostatin receptors, facilitating effective imaging when complexed with technetium-99m (99mTc-depreotide). This compound plays a crucial role in somatostatin receptor imaging, aiding in the diagnosis and research of various tumors. Additionally, depreotide can be employed in the synthesis and investigation of Radionuclide-Drug Conjugates (RDCs) for targeted therapeutic applications. -
Somatostatin Receptor Activator
Reltecimod is a somatostatin receptor activator that modulates the immune response by targeting the CD28/B7-2 co-stimulatory pathway. This compound exhibits protective effects against various bacterial infections, their toxins, and ionizing radiation. Reltecimod is particularly relevant for research into necrotizing soft-tissue infections (NSTIs), providing insights into therapeutic interventions and immune modulation. -
D2R/SSTR2 Agonist
Onzigolide is a chimeric compound that acts as a potent agonist at dopamine type 2 (D2R) and somatostatin type 2 (SSTR2) receptors. This dual receptor activation may play a crucial role in modulating neuroendocrine and neurological functions. It is particularly relevant in research focused on neuropsychiatric disorders and endocrine-related conditions, contributing to the understanding of receptor interactions and their implications in therapeutic contexts. -
sst2/sst5 Receptor Partial Agonist
Angiopeptin is a cyclic octapeptide analogue of somatostatin that acts as a partial agonist at the sst2 and sst5 receptors, exhibiting IC50 values of 0.26 nM and 6.92 nM, respectively. This compound effectively inhibits growth hormone secretion and reduces insulin-like growth factor-1 (IGF-1) production. Angiopeptin also modulates cellular signaling by inhibiting adenylate cyclase and stimulating extracellular acidification. Its unique properties make it a valuable tool for research into coronary atherosclerosis and related metabolic disorders. -
sst1 Agonist
L-797591 hydrochloride is a selective somatostatin receptor 1 (sst1) agonist. It effectively mimics the action of somatotropin release inhibiting factor (SRIF) analogs, SRIF-14 and SRIF-28, by potently inhibiting cAMP accumulation stimulated by Forskolin or corticotropin-releasing hormone (CRH). This compound is useful for studies focused on somatostatin receptor signaling and its implications in neuroendocrine regulation. -
SSTR4 Agonist
SSTR4 Agonist 6 is a selective agonist for the somatostatin receptor subtype 4 (SSTR4), which plays a crucial role in modulating neuroendocrine functions and pain pathways. This compound has demonstrated significant biological activity in preclinical models, making it a valuable tool for investigating the mechanisms of pain and potential therapeutic applications in pain management research. -
MMP Inhibitor
Sucrose octasulfate is a matrix metalloproteinase (MMP) inhibitor that modulates cellular activities by regulating the extracellular matrix. It promotes the release of somatostatin-like immunoreactivity from gastric D cells, facilitating ulcer healing through increased endogenous somatostatin levels. This compound has demonstrated efficacy in improving wound closure in diabetic foot ulcers and venous leg ulcers, making it pertinent for research in chronic wound healing and gastrointestinal disorders. Additionally, sucrose octasulfate serves as a valuable pharmaceutical excipient in various therapeutic applications. -
SST4 Receptor Agonist
J-2156 TFA is a potent and selective agonist of the somatostatin receptor type 4 (SST4), exhibiting IC50 values of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. This compound demonstrates significant anti-inflammatory activity and is utilized in research focused on alleviating mechanical allodynia and mechanical hyperalgesia in rodent models. Its specificity for the SST4 receptor makes it an essential tool in studies related to pain mechanisms and somatostatin signaling pathways. -
SSTR4 Agonist
Mazisotine is a potent agonist of somatostatin receptor 4 (SSTR4) with an EC50 of 4.7 nM. This orally active compound demonstrates significant analgesic properties in models of nociceptive and neuropathic pain, including inflammatory and osteoarthritic conditions. Mazisotine serves as a valuable tool for pain research applications, facilitating the exploration of SSTR4-mediated pathways in pain modulation. -
Somatostatin Receptor Antagonist
Cyclosomatostatin is a potent somatostatin receptor antagonist that specifically targets somatostatin receptor type 1 (SSTR1). This compound effectively inhibits SSTR1 signaling, leading to reduced cell proliferation, decreased ALDH+ cell population size, and diminished sphere formation in colorectal cancer cells. It serves as a valuable tool for research applications focused on understanding the role of somatostatin signaling in cancer biology. -
SST Agonist
CH 275 is a peptide analog of somatostatin that selectively targets somatostatin receptor 1 (sst1) with a Ki of 52 nM. As a potent sst1 agonist, it exhibits an IC50 of 30.9 nM while demonstrating much lower affinities for human sst3, sst4, sst2, and sst5, with IC50 values of 345 nM, >1 μM, >10 μM, and >10 μM, respectively. CH 275 is valuable for researching the role of somatostatin in Alzheimer's disease and other neurodegenerative disorders. -
Neuropeptide
Cortistatin 14 is a neuropeptide that primarily targets somatostatin receptors (SSTRs) and the ghrelin receptor. This compound exhibits neuronal depressant and sleep-modulating properties, making it vital for studies related to sleep physiology and neural signaling. Additionally, its presence alongside GABA in the cortex and hippocampus highlights its role in modulating neurotransmission and potential applications in researching sleep disorders and neurodegenerative conditions. -
SSTR1/SSTR4 Agonist
TT-232 is a somatostatin derivative that acts as an agonist for the somatostatin receptors SSTR1 and SSTR4. This compound has been shown to inhibit cancer cell proliferation and induce apoptosis, making it a significant candidate for cancer research. Additionally, TT-232 exhibits broad-spectrum anti-inflammatory and analgesic properties, supporting its use in studies related to inflammation and pain management. -
Somatostatin Neuropeptide
Cortistatin-17 (human) is a somatostatin neuropeptide that modulates neuroendocrine signaling through its interaction with somatostatin receptors. Its biological activities include the regulation of endocrine and exocrine functions, as well as potential anti-inflammatory effects. This peptide is valuable for research applications related to cancer, inflammation, autoimmunity, fibrosis, and pain. -
hsst2 Antagonist
PRL 2915 is a potent antagonist of the human somatostatin subtype 2 receptor (hsst2), exhibiting a Ki value of 12 nM. This compound effectively inhibits hsst2-mediated signaling pathways, making it a valuable tool for studying somatostatin-related physiological processes and disorders. Its application in research may contribute to a better understanding of neuroendocrine regulation and potential therapeutic approaches in related diseases. -
Somatostatin Receptor Antagonist
BIM-23056 is a linear octapeptide that acts as a potent antagonist of somatostatin receptors sst3 and sst5, exhibiting Ki values of 10.8 nM and 5.7 nM, respectively. This compound is valuable for research into somatostatin signaling pathways and their role in various physiological and pathological conditions. Applications include studies in neuroendocrinology and potential therapeutic investigations targeting somatostatin-related disorders. -
sst4 Receptor Agonist
L-803087 is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM, which demonstrates over 280-fold selectivity compared to other somatostatin receptors. This compound is known to enhance AMPA-mediated hippocampal synaptic responses in vitro and has been shown to increase kainate-induced seizures in murine models. L-803087 is a valuable tool for investigating the pharmacological roles of sst4 receptors in neurological research. -
Somatostatin Receptor Antagonist
SRA880 is a selective antagonist of the somatostatin receptor subtype sst(1). This non-peptide compound has demonstrated antidepressant-like effects, particularly in conjunction with Imipramine. SRA880 can be utilized in research applications focused on mood disorders and somatostatin signaling pathways, contributing valuable insights into potential therapeutic mechanisms.
