Catalog No.
Product Name
Application
Product Information
Citations
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Neuropeptide
Cortistatin-29 is a rat neuropeptide that targets somatostatin receptors (SSTRs) with high affinity, exhibiting IC50 values of 2.8 nM for SSTR1, 7.1 nM for SSTR2, 0.2 nM for SSTR3, 3.0 nM for SSTR4, and 13.7 nM for SSTR5. This compound is known to alleviate neuropathic pain and demonstrates anti-fibrotic properties. Its diverse biological activities make it a valuable tool for research in neurobiology and fibrosis-related studies. -
SSTR5 Antagonist
SSTR5 antagonist 6 is a selective antagonist for somatostatin receptor subtype 5 (SSTR5), exhibiting an IC50 of 24 nM. This compound plays a significant role in modulating signaling pathways associated with glucose homeostasis and insulin regulation, making it valuable for research related to type 2 diabetes. Its oral bioactivity enhances its potential for in vivo studies, facilitating exploration of SSTR5's impact on metabolic disorders. -
SST1 Antagonist
SST1 receptor antagonist-1 is a selective antagonist of the Somatostatin receptor 1 (SST1), exhibiting pKds of 9.11 and 8.79 for rat and human SST1, respectively. This compound is utilized in research focused on retinal and endocrine dysfunctions, as well as cancer and neuropsychiatric disorders, making it a valuable tool for investigating the role of SST1 in various biological systems. -
sstr3 Antagonist
MK-1421 is a potent and selective antagonist of the somatostatin receptor type 3 (sstr3). By inhibiting sstr3, MK-1421 plays a significant role in the modulation of insulin secretion, making it a valuable tool in research related to type 2 diabetes. Its specificity and efficacy make it suitable for investigating the complex pathways involved in metabolic disorders. -
Somatostatin Analogue
[D-Trp8,Tyr11] Somatostatin is a somatostatin analogue that enhances the hormone's stability and bioactivity. This compound is known to inhibit the secretion of growth hormone and other hormones, making it valuable in studies related to hormonal regulation and physiological processes. Applications include endocrynology research and the investigation of tumor growth inhibition, particularly in neuroendocrine tumors. -
Somatostatin-28 (1-14) Analogue
[Tyr12] Somatostatin 28 (1-14) is an analogue of Somatostatin-28 (1-14) that targets somatostatin receptors to modulate neuropeptide signaling. This peptide fragment plays a crucial role in the regulation of various physiological processes, including hormone secretion and cell proliferation. It is commonly used in research applications focused on neuroendocrine signaling pathways and therapeutic interventions for endocrine-related disorders. -
SSTR4 Agonist
SSTR4 Agonist 3 is a selective agonist for the somatostatin receptor subtype 4 (SSTR4), which is primarily expressed in the hippocampus and neocortex, areas implicated in memory and learning. This compound demonstrates significant biological activity in rodent models, exhibiting anti-nociceptive and anti-inflammatory effects that are relevant to both acute and chronic pain conditions. SSTR4 Agonist 3 holds potential for further research into pain modulation and Alzheimer's disease pathology. -
Tetradecapeptide
[D-Trp8] Somatostatin-14 is a tetradecapeptide analog of somatostatin that exhibits enhanced potency compared to its native counterpart. This compound primarily targets somatostatin receptors, influencing various physiological processes including hormonal secretion and cell proliferation. It is utilized in research applications focusing on neuroendocrine regulation and the therapeutic potential of somatostatin analogs in treating conditions such as acromegaly and neuroendocrine tumors. -
Dimer Parallel
Octreotide dimer (parallel) is a parallel dimer of Octreotide, a synthetic octapeptide that acts as an agonist of somatostatin receptors. This compound exhibits potent inhibitory effects on hormone secretion, making it valuable for research in neuroendocrine tumors and diagnostic imaging. Octreotide dimer (parallel) is employed in studies exploring endocrine regulation and potential therapeutic applications in various somatostatin receptor-related disorders. -
Somatostatin Analog
AP102 is a dual somatostatin receptor analogue targeting SSTR2 and SSTR5. This disulfide-bridged octapeptide exhibits subnanomolar affinity for SSTR2 and SSTR5, with IC50 values of 0.63 nM and 0.65 nM, respectively, while showing no binding to SSTR1 or SSTR3. AP102 is particularly valuable in research related to acromegaly and neuroendocrine tumors, providing insights into receptor-specific signaling pathways. -
sst2 Agonist
(1R,1'S,3'R/1R,1'R,3'S)-L-054,264 is a selective non-peptide agonist for the human somatostatin receptor subtype 2 (sst2). This compound is instrumental in investigating the role of sst2 in retinal neuromodulation, making it valuable for research on neurobiology and related therapeutic applications. Its unique selectivity allows for precise modulation of receptor activity, facilitating studies on somatostatin-mediated pathways. -
sst4 Receptor Agonist
L-803087 TFA is a potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. Demonstrating over 280-fold selectivity for the sst4 receptor compared to other somatostatin receptors, L-803087 TFA enhances AMPA-mediated synaptic responses in the hippocampus. This compound is also noted for its role in increasing kainate-induced seizures in murine models, making it valuable for research into neurophysiological processes and receptor signaling mechanisms. -
SST1 Antagonist
SST1 receptor antagonist-2 is a piperazine derivative that selectively inhibits somatostatin receptor 1 (SST1). This compound displays significant potential in the investigation of psychiatric disorders, neurodegenerative diseases, tumors, vascular conditions, and immunological diseases. Its selective antagonism of SST1 may provide insights into various pathological processes and therapeutic strategies. -
SSTR2 Agonist
Branosotine is a potent agonist of the somatostatin receptor subtype 2 (SSTR2), exhibiting an EC50 of less than 0.1 nM. This compound demonstrates significant biological activity in modulating neuroendocrine signaling pathways, making it a valuable tool for research involving neuropsychiatric disorders and hormonal regulation. Its high specificity and efficacy position Branosotine as an important reagent for studying SSTR2-related biological processes. -
Somatostatin Receptor Agonist
Zavolosotine is an orally active agonist of the somatostatin receptor type 5 (SST5), exhibiting a potent EC50 of less than 1 nM. This compound effectively inhibits insulin and glucagon secretion while also elevating glucagon levels in a rat model. Zavolosotine is valuable for research in glucose metabolism and endocrine signaling pathways, making it a key reagent for studies on metabolic disorders and diabetes. -
SSTR4 Agonist
Mazisotine tartrate is a potent SSTR4 agonist that selectively activates the somatostatin receptor subtype 4. This compound is primarily involved in modulating neuroendocrine functions and has potential applications in the study of metabolic disorders, neuroprotection, and cancer therapy. Its biological activity suggests utility in investigating signaling pathways linked to this receptor subtype, making it a valuable tool for research in endocrinology and related fields. -
SSTR5 Antagonist
SSTR5 Antagonist 3 is a potent inhibitor targeting the somatostatin receptor subtype 5 (SSTR5) with IC50 values of 2.8 nM in human tissues and 1.4 nM in mouse models. This orally bioavailable compound exhibits low hERG inhibition, making it suitable for in vivo studies. SSTR5 Antagonist 3 is primarily utilized in research focusing on anti-gallstone therapies and the modulation of related gastrointestinal functions. -
Somatostatin
Tyr-Somatostatin-28 is a potent somatostatin analog featuring a tyrosine residue at the N-terminus. This modification enhances its stability and bioactivity, making it an important tool for studying somatostatin receptor interactions and signaling pathways. Tyr-Somatostatin-28 has applications in neurobiology and endocrinology research, particularly in the investigation of hormone regulation and therapeutic targets for diseases such as acromegaly and neuroendocrine tumors. -
sst2 Receptor Agonist
BIM-23027 is a selective agonist of the sst2 receptor, exhibiting an EC50 of 0.32 nM. This compound mimics the action of somatostatin (SRIF), a cyclic tetradecapeptide, and plays a critical role in stimulating dopamine release through a Glu-dependent mechanism. BIM-23027 is suitable for research applications focusing on neuroendocrine regulation and receptor pharmacology. -
Somatostatin Analogue
DOTAMTATE is a somatostatin analogue that selectively targets somatostatin receptors. It exhibits significant potential for the imaging and treatment of somatostatin receptor-positive neuroendocrine tumors, making it a valuable tool for investigative research in oncology and radiopharmaceutical applications. The incorporation of 212Pb into DOTAMTATE enhances its therapeutic efficacy and suitability for targeted radionuclide therapy. -
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.
- 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. - Somatostatin is an endogenous peptide noted to inhibit the release of growth hormone, insulin and glucagon.
- 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 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). -
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 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). -
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. -
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. -
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. -
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.
