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RXFP1 Receptor Agonist
RXFP1 receptor agonist-5 is a selective agonist for the RXFP1 receptor, a key regulator of various physiological processes. This compound effectively stimulates cAMP production in HEK293 cells that stably express the human RXFP1 receptor, demonstrating an EC50 value of 1.3 nM. It is an invaluable tool for research applications involving signal transduction, reproductive biology, and cardiovascular studies. -
Relaxin Receptor Agonist
Efranarelaxin alfa acts as a relaxin receptor agonist, primarily influencing cardiovascular health and tissue regeneration pathways. This compound has potential applications in research focused on cardiovascular diseases and promoting tissue repair mechanisms, offering a valuable tool for exploring therapeutic strategies in these areas. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-3 is a selective agonist for the RXFP1 receptor, known to enhance the production of cyclic AMP (cAMP) in HEK293 cells that stably express the human RXFP1. With an effective concentration (EC50) of 2 nM, RXFP1 receptor agonist-3 serves as a valuable tool for studying the biological functions and signaling pathways associated with RXFP1, facilitating research in areas such as cardiovascular biology and neurobiology. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-2 is a potent agonist of the RXFP1 receptor, demonstrating the ability to stimulate cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1 nM. This compound is useful for investigating the role of the RXFP1 receptor in various physiological processes and cellular signaling pathways. It serves as a valuable tool in pharmacological research focused on receptor function and related biological activities. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-7 is a selective agonist of the RXFP1 receptor, facilitating significant increases in cAMP production. This compound has demonstrated an EC50 value of 4.2 nM in HEK293 cells stably expressing human RXFP1, indicating potent activity. RXFP1 receptor agonist-7 is suitable for research applications focusing on signal transduction, neurobiology, and cardiovascular studies involving the RXFP1 pathway. -
RXFP3/4 Agonist
RXFP3/4 Agonist 1 is a selective agonist of the relaxin family peptide 3/4 receptors (RXFP3/4), exhibiting EC50 values of 82 nM for RXFP3 and 2 nM for RXFP4. This compound has been shown to enhance food intake in rat models, making it a valuable tool for studying appetite regulation and metabolic processes. Its potency and specificity make it suitable for research focusing on the roles of RXFP3/4 in energy homeostasis and related signaling pathways. -
RXFP1 Agonist
RXFP1 receptor agonist-9 is a selective agonist for the RXFP1 receptor, displaying an EC50 of 2.5 μM and a maximum response (Ymax) of 65%. This compound demonstrates excellent microsomal stability along with favorable pharmacokinetic properties, making it suitable for in vivo studies. RXFP1 receptor agonist-9 is primarily utilized in the investigation of heart failure and related cardiovascular conditions. -
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. -
Agonist of sst3 Receptor
L-796778 acetate is a selective agonist of the sst3 receptor. It acts as a partial agonist in CHO-K1 cells expressing the human sst3 receptor, effectively inhibiting Forskolin-stimulated cAMP production with an IC50 of 18 nM. Additionally, L-796778 acetate demonstrates anticonvulsant properties, making it a valuable tool for research in neurological studies and receptor signaling pathways. -
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. -
SSTR Agonist
Veldoreotide TFA is a somatostatin analogue that acts as an agonist for somatostatin receptors (SSTR) 2, 4, and 5. This compound effectively inhibits growth hormone (GH) secretion in adenomas, demonstrating enhanced efficacy compared to other somatostatin analogues. Additionally, Veldoreotide TFA shows promise as a pain-modulating agent, making it valuable in research applications related to endocrine and pain pathways. -
Somatostatin Receptor Agonist
Somatostatin-28 (1-14) serves as an agonist of somatostatin receptors. This N-terminal fragment of the neuropeptide somatostatin-28 plays a critical role in regulating various physiological processes, including hormone secretion and neurotransmission. It is widely used in research applications investigating metabolic regulation, neurobiology, and potential therapeutic strategies for neuroendocrine disorders. -
Antineoplastic Agent
Lanreotide is a somatostatin analogue that exhibits antineoplastic properties by inhibiting growth hormone and other peptide hormone secretions. It is primarily utilized in the study of carcinoid syndrome and other neuroendocrine tumors due to its ability to suppress tumor growth and hormonal activity. This compound provides a valuable tool for researchers investigating hormone-related cancers and their management. -
SSTR5 Antagonist
SSTR5 antagonist 2 hydrochloride is a potent and selective antagonist of the somatostatin receptor subtype 5 (SSTR5). This compound demonstrates significant biological activity in modulating SSTR5 signaling pathways, making it a valuable tool for investigating the role of somatostatin in various physiological and pathological processes. It is particularly relevant for research applications related to type 2 diabetes mellitus (T2DM) and other metabolic disorders. -
Somatostatin Receptor Agonist
L-817818 is a potent and subtype-selective agonist of the somatostatin receptor. This compound facilitates the exploration of somatostatin receptor physiological functions, contributing to a better understanding of its role in various biological processes. It is useful for research applications aimed at studying neuroendocrine regulation and potential therapeutic targets related to somatostatin signaling. -
SSTR2 Agonist
Seglitide acetate is a potent agonist of the somatostatin receptor 2 (SSTR2) and serves as a competitive antagonist of SSTR14, SSTR25, and SSTR28. It exhibits significant antihypertensive properties and has the capability to inhibit plasma glucagon and growth hormone levels. This compound is valuable for research applications related to diabetes and metabolic disorders. -
Somatostatin Neuropeptide
Cortistatin-29 (human) is a somatostatin neuropeptide that modulates a variety of biological functions by interacting with somatostatin receptors. This compound exhibits key biological activities, including anti-inflammatory effects and regulation of pain pathways, making it relevant for research applications in cancer, inflammation, autoimmunity, fibrosis, and pain management. Its unique biological profile allows for exploration of potential therapeutic strategies targeting these conditions. -
sst4 Agonist
NNC 26-9100 is a selective full agonist of the somatostatin sst4 receptor, exhibiting a Ki of 6 nM and an EC50 of 2 nM. This compound has been demonstrated to reduce total soluble Aβ42 levels while increasing neprilysin activity in the brain, suggesting a potential role in neuroprotection. NNC 26-9100 may be valuable for research applications focused on neurodegenerative disorders and cognitive enhancement. -
SSTR4 Agonist
SSTR4 Agonist 2 is a selective agonist of the somatostatin receptor subtype 4 (SSTR4), which plays a critical role in modulating nociceptive and inflammatory pathways. This compound exhibits significant biological activity by engaging the SSTR4 pathway, making it a valuable tool for investigating medical disorders associated with SSTR4 dysfunction. Its potential research applications include studying pain mechanisms and inflammation regulation. -
Somatostatin Receptors Activator
Veldoreotide is a somatostatin receptor activator that selectively binds to and activates somatostatin receptors 2, 4, and 5. This compound effectively inhibits growth hormone secretion in adenomas, presenting a potential advantage over other somatostatin analogues. Additionally, Veldoreotide may serve as a pain modulating agent, making it relevant for research in endocrine disorders and pain management strategies. -
Neuroavtive Peptide
[Tyr11]-Somatostatin is a neuroactive peptide that modulates various physiological processes by targeting somatostatin receptors. This compound is essential for studying the role of neuroactive substances in retinal physiology and their implications in various neurobiological research applications. Its use in proteomics research contributes to a deeper understanding of neuronal signaling pathways and potential therapeutic targets. -
SSTR2 Agonist
Seglitide, a potent agonist of the somatostatin receptor 2 (SSTR2), exhibits important biological activities including antihypertensive effects and the inhibition of plasma glucagon and growth hormone. This compound also acts as a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide is valuable for research focusing on diabetes and related metabolic disorders, providing insights into somatostatin signaling pathways and their therapeutic potential. -
Somatostatin Agonist
Pasireotide pamoate is a long-acting somatostatin analogue that primarily targets somatostatin receptors (sst1/2/3/4/5) with notable binding affinity (pKi=8.2/9.0/9.1/<7.0/9.9). This compound demonstrates significant antisecretory, antiproliferative, and proapoptotic properties, making it valuable for research on neuroendocrine tumors and disorders related to dysregulated hormone secretion. Its diverse biological activities support investigations into therapeutic approaches for various endocrine-related pathologies. -
Somatostatin (1-28) Derivative
[Nle8] Somatostatin (1-28) is a derivative of somatostatin (1-28) in which norleucine substitutes for methionine at position 8. This compound enhances amylase release and elevates cyclic AMP levels in pancreatic acini. It is utilized in research to study pancreatic function and the regulatory mechanisms of peptide hormones in metabolic processes. -
Somatostatin Enhancer
FK962 is a somatostatin enhancer that stimulates the release of this neuropeptide, leading to cognitive-enhancing effects. Its potential anti-dementia properties make it a valuable compound for research focused on neurological diseases and cognitive disorders. Studies exploring FK962 may contribute to a better understanding of somatostatin's role in neuroprotection and cognitive function. -
MMP Inhibitor
Sucrose octasulfate sodium is a potent matrix metalloproteinase (MMP) inhibitor that enhances the release of somatostatin-like immunoreactivity (SLI) from gastric D cells. This compound promotes ulcer healing by increasing endogenous gastric somatostatin levels. Sucrose octasulfate sodium is utilized in research related to chronic wound healing and has shown significant efficacy in improving wound closure in diabetic foot ulcers and venous leg ulcers. Additionally, it serves as a useful pharmaceutical excipient in various applications. -
Somatostatin Receptor Antagonist
PRL 3195 is a somatostatin receptor antagonist that exhibits inhibition constants (Kis) of 6, 17, 66, 1000, and 1000 nM for human somatostatin receptors sst5, sst2, sst3, sst1, and sst4, respectively. This compound is utilized in research to investigate the role of somatostatin signaling in various physiological and pathological processes. Its selective blockade of somatostatin receptors makes it a valuable tool for studying neuroendocrine regulation and potential therapeutic applications in disorders involving somatostatin dysregulation. -
SSTR3 Agonist
SSTR3 Agonist-1 is a selective agonist for the somatostatin receptor subtype 3 (SSTR3), exhibiting an EC50 value of 0.14 nM. This compound has demonstrated efficacy in reducing kidney cystic index, making it a valuable tool in studying autosomal dominant polycystic kidney disease. SSTR3 Agonist-1 facilitates research into therapeutic strategies targeting SSTR3 and its role in renal pathophysiology. -
Somatostatin Receptor 5 Agonist
BIM 23052 is a selective agonist for the somatostatin receptor 5 (SSTR5). It has been shown to enhance gastric emptying, making it a valuable tool for research in gastrointestinal function and disorders. This compound is of particular interest in studies investigating the regulatory mechanisms of hormone action and potential therapeutic applications in gastric motility disorders. -
Antineoplastic Agent
Lanreotide diTFA is a somatostatin analogue that exhibits antineoplastic activity by inhibiting the secretion of growth hormone and other hormones in neuroendocrine tumors. This compound is primarily utilized in research related to carcinoid syndrome and other neuroendocrine disorders. Its mechanism of action involves receptor binding that modulates neuroendocrine function, making it a valuable tool in oncology research. -
Somatostatin Receptor
[Tyr1]-Somatostatin-14 is a bioactive peptide that specifically targets the somatostatin receptor subtype 2 (SSTR2). This compound exhibits high binding affinity, making it a crucial tool for studying receptor signaling pathways and somatostatin-mediated biological processes. Its applications extend to cancer research, neurobiology, and endocrine function studies, allowing researchers to explore therapeutic interventions and physiological mechanisms involving somatostatin receptors. -
Somatostatin Analog
(D-Phe5,Cys6,11,N-Me-D-Trp8)-Somatostatin-14 (5-12) amide is a somatostatin analog that demonstrates selective binding affinity with Kd values of 0.61 nM for SSTR5, 11.05 nM for SSTR3, 23.5 nM for SSTR2, 1200 nM for SSTR1, and >1000 nM for SSTR4. This compound exhibits significant biological activity relevant to the regulation of hormonal secretion and inhibition of tumor growth. It is suitable for research applications investigating the role of somatostatin receptors in various physiological and pathological processes. -
Human Somatostatin Receptor Antagonist
BN-81674 is a selective antagonist targeting the human somatostatin sst3 receptor, exhibiting a Ki of 0.92 nM. This compound effectively reverses the inhibition of cyclic AMP accumulation caused by somatostatin at nanomolar concentrations, with an IC50 value of 0.84 nM. BN-81674 is suitable for applications in cancer research, particularly in studies assessing somatostatin signaling pathways and their implications in tumor biology. -
Somatostatin-28 Analog
[Leu8,D-Trp22,Tyr25] Somatostatin-28 is an analog of somatostatin-28, a peptide that plays a critical role in inhibiting hormone secretion and regulating various physiological functions. This modified form enhances the stability and potency of its biological activity, making it useful in research related to neuroendocrine signaling and metabolic regulation. Applications include studying cell signaling pathways, hormonal regulation, and potential therapeutic effects on neuroendocrine tumors. -
SSTR5 Antagonist
SSTR5 antagonist 4 is a highly potent and selective antagonist of the somatostatin subtype 5 receptor (SSTR5), exhibiting IC50 values of 1.3 nM for human SSTR5 and 1.0 nM for mouse SSTR5. This compound demonstrates significant efficacy in the mouse oral glucose tolerance test (OGTT) in high fat diet-induced mice. SSTR5 antagonist 4 is a valuable tool for research into type 2 diabetes and related metabolic disorders. -
SSTR4 Agonist
SSTR4 Agonist 4 is a potent agonist of the somatostatin receptor 4 (SSTR4), which is predominantly expressed in the hippocampus and neocortex, areas crucial for memory and learning. This compound demonstrates significant anti-nociceptive and anti-inflammatory activity in rodent models of both acute and chronic pain. SSTR4 Agonist 4 holds potential for advancing research into pain mechanisms and therapeutic interventions for conditions such as Alzheimer's disease. -
SSTR1 Agonist
L-797591 is a selective agonist of the somatostatin receptor subtype 1 (SSTR1). This compound has demonstrated significant biological activity in modulating neuroendocrine signaling pathways and can be utilized in research focused on neurobiology, cancer biology, and metabolic disorders. Its ability to selectively activate SSTR1 makes it a valuable tool for investigating the physiological and therapeutic roles of somatostatin receptors in various biological systems. -
SRIF Antagonist
AC-178335 is a selective antagonist of somatostatin receptor type 2 (SRIF), exhibiting a Ki value of 172 nM. It effectively inhibits the SRIF-mediated suppression of adenylate cyclase with an IC50 of 5.1 μM in vitro. This compound has demonstrated the capability to induce growth hormone release in anesthetized rat models, making it a valuable tool for investigating the physiological role of somatostatin signaling in endocrine regulation.

