Catalog No.
Product Name
Application
Product Information
Citations
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ACU Inhibitor/VR1 Agonist
OMDM-5 is a selective anandamide cellular uptake (ACU) inhibitor, exhibiting a Ki of 4.8 μM. In addition, OMDM-5 demonstrates potent activity as a vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM. This compound also shows weak activity as a cannabinoid receptor type 1 (CB1) ligand, with a Ki of 4.9 μM. Its properties make OMDM-5 useful for studies involving pain modulation and endocannabinoid signaling pathways. -
Exenatide Impurity
(D-Asn28)-Exenatide is an impurity of Exenatide, which functions as a long-acting agonist of the glucagon-like peptide-1 receptor. This compound may be used in research applications focusing on peptide synthesis, quality control, and pharmacological studies involving GLP-1 receptor pathways. Its significance lies in understanding the properties and effects of Exenatide-related compounds. -
RGS Protein Inhibitor
CCG 203769 is a selective inhibitor of the regulator of G protein signaling (RGS4), effectively disrupting the RGS4-Gαo protein-protein interaction with an IC50 of 17 nM. This compound is instrumental for research applications focused on G protein-coupled signaling pathways and the modulation of G protein activity. CCG 203769 may be utilized in studies exploring the role of RGS proteins in various physiological processes and disease states. -
RGS Agonist
BMS-192364 is a selective RGS (Regulator of G Protein Signaling) agonist that targets the Gα-RGS interaction, promoting the formation of an inactive Gα-RGS complex. This compound has been shown to reduce urinary bladder contraction and enhance the activity of GTPase-activating proteins (GAPs) on Gq proteins. Additionally, BMS-192364 inhibits calcium flux, making it a valuable tool for studying signaling pathways involved in bladder function and related physiological processes. -
RGS10 Modulator
RGS10 modulator-1 functions as a potent modulator of the RGS10 protein, exhibiting significant biological activity by reversing interferon-gamma (IFNγ)-induced expression of RGS10 protein and mRNA. Additionally, this compound effectively reduces the levels of COX-2 mRNA and inducible nitric oxide synthase (iNOS) expression that are stimulated by IFNγ. RGS10 modulator-1 is a valuable tool for research exploring the regulatory mechanisms of RGS10 in inflammatory responses and related signaling pathways. -
RGS14 Inhibitor
Z55660043 is a selective inhibitor of Regulator of G protein Signaling-14 (RGS14) with an IC50 of 2.3 μM. This compound acts by non-covalently inhibiting the GTPase-accelerating protein (GAP) activity of RGS14, demonstrating a favorable safety profile without significant cytotoxic effects. Z55660043 is suitable for research focused on central nervous system and metabolic disorders, contributing to the understanding of RGS14's role in these biological processes. -
RGS4 Inhibitor
CCG-2046 is a selective inhibitor of the regulator of G-protein signaling 4 (RGS4), demonstrating an IC50 value of 4.3 μM for inhibiting the RGS4-Gαo interaction. This compound modulates G-protein signaling pathways, making it a valuable tool for studying their role in various physiological processes. CCG-2046 is suitable for research applications focused on neurobiology, cardiac function, and potential therapeutic interventions for related disorders. -
RGS Protein Inhibitor
CCG-4986 is a selective RGS protein inhibitor that covalently modifies the Cys-132 residue of RGS4, thereby inhibiting its activity. This compound is valuable for studying the implications of altered G protein-coupled receptor (GPCR) signaling in various pathological conditions, including Parkinson's disease and opioid addiction. CCG-4986 is a useful tool for researchers investigating the role of RGS proteins in cellular signaling pathways. -
RXFP1 Modulator
AZD5462 is an RXFP1 modulator that targets the relaxin receptor, which is part of the GPCR family. This compound exhibits anti-fibrotic and anti-inflammatory properties, making it a valuable tool for research into heart failure and related cardiovascular diseases. Its application in studies of RXFP1 signaling pathways can provide insights into potential therapeutic strategies for heart dysfunction. -
RXFP2 Agonist
RXFP2 Agonist 2 is a selective allosteric agonist of the RXFP2 receptor, exhibiting an EC50 of 0.38 μM. This compound promotes osteoblast mineralization and enhances bone formation in female mice. RXFP2 Agonist 2 is valuable for research studies focused on osteoporosis and bone health. -
RXFP3/4 Agonist
RXFP3/4 Agonist 2 is a potent nonpeptide dual agonist targeting RXFP3 and RXFP4, with EC50 values of 3.1 nM and 2.7 nM, respectively. This compound effectively promotes the interaction between RXFP3 and β-arrestin-2, displaying EC50 values ranging from 10 to 22 nM. RXFP3/4 Agonist 2 is valuable for investigating receptor signaling pathways and exploring potential therapeutic applications related to metabolic and cardiovascular diseases. -
RXFP4 Agonist
A13:B7-24-GG is a selective RXFP4 agonist that acts through its high-affinity binding (Ki = 2.29 nM) to the RXFP4 receptor, while demonstrating minimal interaction with RXFP3 (Ki = 602.56 nM). This compound effectively inhibits cAMP production with an EC50 of 1.17 nM and facilitates the recruitment of β-Arrestin2, showing an EC50 of 22.39 nM. A13:B7-24-GG is primarily utilized in research focused on chronic constipation and related gastrointestinal disorders. -
RXFP1 Agonist
AZ7976 is a highly selective agonist for the Relaxin Family Peptide Receptor 1 (RXFP1), displaying a pEC50 value greater than 10.5. This compound enhances cAMP signaling through an allosteric mechanism, resulting in a physiological increase in heart rate. AZ7976 is suitable for investigations in cardiovascular disease research and related studies focusing on RXFP1-mediated pathways. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-6 is a potent agonist of the RXFP1 receptor, effectively stimulating cAMP production in HEK293 cells that stably express the human RXFP1. With an EC50 value of 12 nM, this compound is valuable for research applications focused on understanding RXFP1 signaling pathways and their implications in various physiological processes. -
RXFP2 Agonist
RXFP2 Agonist 1 selectively targets the relaxin family peptide receptor 2 (RXFP2) and demonstrates potent agonistic activity with an EC50 of 0.06 µM. This compound plays a significant role in cellular signaling pathways associated with bone metabolism and has potential applications in osteoporosis research. Its ability to modulate RXFP2 activity makes it a valuable tool for studies focused on therapeutic strategies aimed at bone health and regeneration. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-10 is a potent RXFP1 receptor agonist with an EC50 value of 0.5 nM. This compound exhibits significant biological activity, making it a valuable tool for studying the physiological roles of the RXFP1 receptor. Its utility in research extends to investigations related to heart failure, providing insights into the potential therapeutic mechanisms involving RXFP1 modulation. -
RXFP1 Activator
Efadirelaxin alfa is a selective agonist of the relaxin/insulin-like family peptide receptor RXFP1, exhibiting a prolonged terminal half-life following subcutaneous administration. It demonstrates significant anti-cardiac hypertrophy and anti-fibrotic properties by modulating the TGF-β1/Smad2 and AKT/eNOS signaling pathways. Efadirelaxin alfa effectively reverses cardiac hypertrophy and collagen deposition while improving cardiac systolic function, all without affecting blood pressure or heart rate. This compound is primarily utilized in research focused on heart failure mechanisms and therapies. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-8 is a selective agonist for the RXFP1 receptor, which plays a crucial role in the modulation of cellular signaling pathways. This compound effectively stimulates cAMP production in HEK293 cells that stably express human RXFP1, exhibiting an EC50 value of 1.8 nM. It is valuable for research applications investigating RXFP1-mediated signaling and its physiological implications. -
RXFP3 Agonist
RXFP3 Agonist 1 is a nonpeptide compound that selectively activates the RXFP3 receptor with an EC50 value of 6937 nM. This reagent is valuable for investigating the physiological roles of RXFP3 in various biological processes, including mood regulation and reproductive functions. Its application extends to studies exploring potential therapeutic targets for diseases associated with RXFP3 signaling pathways. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-4 is a selective agonist for the RXFP1 receptor. It effectively stimulates cyclic AMP (cAMP) production in HEK293 cells that stably express the human RXFP1 receptor, demonstrating an EC50 value of 4.9 nM. This compound is valuable for research applications related to the RXFP1 signaling pathway and its role in various physiological processes. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-1 selectively targets the RXFP1 receptor, leading to the activation of downstream signaling pathways. This compound effectively stimulates cyclic AMP (cAMP) production in HEK293 cells that stably express human RXFP1, demonstrating an EC50 value of 300 nM. It serves as a valuable tool for research into receptor signaling mechanisms and the physiological implications of RXFP1 activation. -
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.
