Catalog No.
Product Name
Application
Product Information
Citations
-
Somatostatin Receptor Agonist
SSTR4 Agonist 5 is a potent, orally active agonist of the somatostatin receptor 4 (SSTR4) with an EC50 value of 0.228 nM. Demonstrating considerable stability in human and rat liver microsomes, this compound has shown effectiveness in inhibiting mechanical hyperalgesia in rat models. It is a valuable tool for research applications involving pain mechanisms and SSTR4-related pathways. -
Somatostatin Receptor Agonist
L-054522 is an agonist for somatostatin receptor subtype 2, featuring a Kd of 0.01 nM. This compound effectively inhibits growth hormone secretion from rat primary pituitary cells with an IC50 of 0.05 nM, as well as glucagon and insulin release from isolated mouse pancreatic islet cells, exhibiting IC50 values of 0.05 nM and 12 nM, respectively. L-054522 serves as a valuable tool for exploring somatostatin signaling and its impact on endocrine functions in research applications. -
Somatostatin Analogue
(D-Trp8,D-Cys14)-Somatostatin-14 is a synthetic analogue of somatostatin, targeting somatostatin receptors. This peptide exhibits significant biological activity in modulating hormonal secretion and inhibiting cell proliferation, making it valuable in research related to metabolic disorders and neuroendocrine tumors. Its unique structure allows for enhanced stability and potency in various biological assays. -
Somatostatin Receptor Inhibitor
Des-threoninol-octreotide is a potent somatostatin receptor inhibitor, primarily targeting the mSSTR2b, rSSTR5, and hSSTR5 receptor subtypes. This compound demonstrates high inhibitory activity with IC50 values of 13.62 nM, 10.63 nM, and 10.95 nM, respectively. It is valuable for research applications exploring neuroendocrine regulation, peptide hormone signaling, and potential therapeutic interventions involving somatostatin pathways. -
Somatostatin Agonist
Pasireotide (diaspartate) is a long-acting somatostatin agonist targeting somatostatin receptors sst1, sst2, sst3, sst4, and sst5, with pKi values of 8.2, 9.0, 9.1, <7.0, and 9.9, respectively. This cyclohexapeptide compound demonstrates significant antisecretory, antiproliferative, and proapoptotic activities. Its diverse biological effects make it a valuable tool for research applications in endocrinology and oncology, particularly in the study of neuroendocrine tumors and hormonal regulation. -
Somatostatin Analogue
Nendratareotide is a somatostatin analogue that primarily targets somatostatin receptors. It exhibits inhibitory effects on hormone secretion, making it valuable in the treatment of neuroendocrine tumors and acromegaly. This compound is also utilized in research focused on understanding the physiological roles of somatostatin and its impact on glucose metabolism and cell proliferation. -
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. -
Urotensin II Anague
Urotensin II-related peptide is an analog of human urotensin II, exhibiting high affinity for the urotensin II receptor (UT). This peptide plays a significant role in cardiovascular regulation and may influence vascular smooth muscle contraction. It is commonly utilized in research focused on cardiovascular diseases, neurobiology, and the study of peptide receptor interactions. -
Urotensin Receptor Antagonist
SB-611812 is a selective antagonist of the urotensin II receptor (UTR), which plays a significant role in cardiovascular regulation. This compound is useful in investigating the pathological mechanisms underlying cardiovascular diseases and may aid in the development of novel therapeutic strategies targeting UTR-mediated pathways. Researchers can utilize SB-611812 to explore its effects on vascular function and cardiac remodeling in experimental models. -
Urotensin II Receptor Antagonist
SB-706375 is an antagonist of the Urotensin II (UII) receptor, which plays a key role in renal physiology. By inhibiting this receptor, SB-706375 effectively decreases the kidney's response to UII and Urotensin-related peptide (URP), leading to a significant increase in Glomerular Filtration Rate (GFR). This compound is valuable for research applications focused on kidney diseases and hypertension, facilitating further understanding of renal function and associated pathologies. -
Urotensin-II Receptor Antagonist
GSK 1562590 hydrochloride is a potent and selective antagonist of the urotensin-II receptor (UT), exhibiting pKi values ranging from 9.14 to 9.66 across various mammalian species, including mouse, rat, cat, monkey, and human. This compound demonstrates significant inhibition of UT-mediated signaling pathways, making it valuable for research into cardiovascular and neuroendocrine disorders associated with urotensin-II. Its high affinity and selectivity position GSK 1562590 as an essential tool for studying the role of urotensin-II in physiological and pathological processes. -
urotensin-II Receptor Antagonist Peptide
Urantide is a selective and competitive antagonist of the urotensin-II (UT) receptor, exhibiting a pKB of 8.3. This peptide effectively inhibits human urotensin-II (hU-II)-induced contractions in rat thoracic aorta ex vivo. Urantide is valuable for investigating the (patho)physiological roles of hU-II in the mammalian cardiovascular system, making it an important tool for related research applications. -
Urotensin Receptor Agonist
Urotensin II (114-124), human, is a peptide comprising 11 amino acids that functions as a potent vasoconstrictor and an agonist for the urotensin receptor (GPR14). This compound is utilized in research to explore cardiovascular function and pathophysiology, particularly regarding its role in regulating vascular tone and blood pressure. Its biological activity makes it a valuable tool for studying urotensin signaling pathways and their implications in various disease states. -
Urotensin II Antagonist
Palosuran hydrochloride is a selective, orally active antagonist of the urotensin II receptor, exhibiting an IC50 of 3.6 nM in CHO cell membranes expressing human recombinant receptors. This compound demonstrates potential to improve pancreatic and renal function in diabetic models, making it a valuable tool for research in metabolic and renal disorders. Its mechanism and target highlight its relevance in studies of urotensin II signaling pathways. -
Urotensin Receptor Agonist
AC-7954 free base is a selective nonpeptidic agonist of the urotensin receptor, demonstrating an EC50 of 300 nM at the human urotensin II receptor. This compound is valuable for research focused on the urotensin signaling pathway and its implications in cardiovascular and metabolic disorders. Its specificity makes it suitable for studies investigating the physiological and pathological roles of urotensin receptors in various biological systems. -
Urotensin Receptor Agonist
AC-7954 is a selective nonpeptidic agonist of the urotensin receptor, exhibiting an EC50 of 300 nM at the human urotensin II receptor. This compound plays a significant role in cardiovascular and metabolic research, with potential applications in the study of hypertension and heart failure. AC-7954 can be utilized to explore urotensin-related signaling pathways and their implications in various physiological processes. -
Urotensin Receptor Antagonist
SB-436811 is a selective antagonist of the urotensin-II receptor, exhibiting a pKi value of 6.7. This compound is primarily utilized in research focused on cardiovascular and metabolic disorders, where the urotensin-II pathway plays a significant role. By inhibiting urotensin-II activity, SB-436811 can aid in the exploration of its physiological effects and potential therapeutic applications. -
Endothelin A Receptor Antagonist
JKC 301 is a selective Endothelin A receptor antagonist that effectively mitigates the pressor effects of nicotine in rat models. This compound is particularly valuable for investigating the cardiovascular diseases associated with smoking. Its targeted mechanism makes JKC 301 a useful tool for researchers studying the pathophysiological effects of nicotine on cardiovascular function. -
Precursor of Endothelin-1
Big Endothelin-1 (1-39), porcine is the precursor peptide of endothelin-1 (ET-1), a potent vasoconstrictor significantly involved in cardiovascular regulation. This reagent exhibits similar pressor effects in vivo, making it valuable for studies investigating vascular function and regulation. It is useful in research applications that aim to elucidate the roles of endothelin peptides in physiological and pathological processes. -
Opioid Receptor Agonist
SR16835 is a selective agonist targeting the nociceptin/orphanin FQ peptide (NOPr) and mu-opioid receptor (MOPr). It exhibits full agonist activity at NOPr and partial agonist activity at MOPr, allowing for detailed exploration of opioid receptor mechanisms. Notably, SR16835 does not produce analgesic effects, making it a valuable tool for research into receptor-specific functions and therapeutic applications in pain management and opioid signaling pathways. -
NOP Receptor Agonist
[Arg14,Lys15]Nociceptin is a highly potent and selective agonist of the NOP receptor (also known as ORL1 or OP4), exhibiting an EC50 of 1 nM. This compound demonstrates exceptional specificity for the NOP receptor, with IC50 values of 0.32 nM for NOP and significantly higher values for μ (280 nM), δ (>10,000 nM), and κ (1500 nM) opioid receptors. [Arg14,Lys15]Nociceptin is valuable for research applications exploring pain modulation, neuropharmacology, and the role of nociceptin in various physiological processes. -
NOP Antagonist
NOP Antagonist 1 is a nociceptin opioid peptide (NOP) antagonist with a binding affinity characterized by a Kb of 8.65 nM. This compound is valuable for research focused on neuropsychiatric disorders, as it modulates nociceptin receptor activity, providing insights into pain signaling and potential therapeutic strategies. Its specificity and potency make it an essential tool for exploring the role of the NOP system in various physiological and pathological conditions. -
μ-opioid Receptor Antagonist
Mu Opioid Receptor Antagonist 8 is a selective antagonist of the μ-opioid receptor. This compound effectively inhibits met-enkephalin-induced activation of the receptor via the Gi signaling pathway, making it valuable for research in pain management and addiction studies. Its ability to modulate μ-opioid receptor activity positions it as a critical tool for understanding opioid receptor pharmacology and potential therapeutic interventions. -
κ Opioid Receptor Agonist
Riminkefon is a κ-opioid receptor agonist that selectively binds to and activates the κ-opioid receptor, leading to various physiological effects. It exhibits significant analgesic properties and has been employed in research related to pain management, mood regulation, and the study of addictive behaviors. Riminkefon serves as a valuable tool for exploring the therapeutic potential of κ-opioid receptor modulation in various neurological and psychological conditions. -
MOR Agonist
SR-14968 is a full allosteric and non-competitive agonist of the mu-opioid receptor (MOR), exhibiting an EC50 of 88 nM in mouse brainstem assays. This compound stabilizes the MOR in a G protein signaling state that demonstrates resistance to washout, while remaining reversible by antagonists. SR-14968 is capable of inducing respiratory depression in murine models, making it a valuable tool for exploring pain-related mechanisms and the pharmacological effects of MOR activation in research settings. -
Kappa-Opioid Receptor Agonist
LPK-26 hydrochloride is a selective kappa-opioid receptor agonist, exhibiting a Ki of 0.68 nM. This compound demonstrates significant antinociceptive properties while showing low potential for physical dependence. It is valuable for research into pain management and the mechanisms of opioid receptor activation. -
µ-Opioid Receptor Agonist
Bilaid A1e is a tetrapeptide that acts as an agonist of the µ-opioid receptor, exhibiting a binding affinity with a Ki value of 750 nM. Isolated from an Australian estuarine strain of Penicillium sp., Bilaid A1e holds potential for applications in pain research. Its ability to modulate µ-opioid receptor activity makes it a valuable tool for studying analgesic pathways and developing pain management strategies. -
Urotensin II Antagonist
Urotensin-II receptor antagonist-1 is a selective antagonist of the human Urotensin II receptor, exhibiting a Ki value of 16 nM in HEK293 cells expressing the recombinant receptor. This compound demonstrates significant biological activity by inhibiting cytochrome P450 enzymes, CYP2D6 and CYP3A4, with IC50 values of 0.75 μM and 1.4 μM, respectively. Additionally, it inhibits the κ-opioid receptor with an EC50 of 3.2 μM and targets cardiac sodium channels with a Ki of 2.5 μM. Research applications include studies of cardiovascular physiology and drug metabolism. -
Opioid Receptor
Faxeladol is an opioid receptor modulator that exhibits significant analgesic activity. In clinical trials, it demonstrated a reduction in mean pain intensity in patients suffering from painful polyneuropathy, supporting its potential as an effective pain management agent. The compound is characterized by a favorable safety profile, making it a candidate for further research in pain relief applications. -
Opioid Receptor Antagonist
LY2048978 is a non-selective opioid receptor antagonist that exhibits Ki values of 0.287 nM, 0.471 nM, and 1.05 nM for human mu, kappa, and delta opioid receptors, respectively. This compound is relevant for studying the physiological roles of opioid receptors and is applied in research related to major depressive disorder and alcohol use disorder. Its antagonistic properties make it a valuable tool for investigating opioid-mediated pathways and potential therapeutic interventions. -
Opioid Agonist
D-Ala2-Met-Enkephalinamide is an opioid peptide that functions as a potent opioid agonist. It exerts analgesic effects and is known to decrease bile flow through central mechanisms. This compound is valuable in research applications focused on pain management and opioid receptor activity. -
Mu-Opioid Receptor Antagonist
Mu Opioid Receptor Antagonist 5 is a selective antagonist of the μ-opioid receptor (MOR) with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. This compound is capable of penetrating the blood-brain barrier, making it a valuable tool for studying the mechanisms underlying opioid use disorders (OUD). Its high potency and specificity for the MOR facilitate insightful research into opioid-related signaling pathways and potential therapeutic interventions. -
Opioid Peptide
Biphalin TFA is a potent opioid peptide analog designed for effective interaction with opioid receptors, demonstrating a dual enkephalin pharmacophore structure that facilitates blood-brain barrier penetration. This compound exhibits significant analgesic properties in various pain models, including acute, neuropathic, and chronic settings. Additionally, Biphalin TFA has been shown to possess antiviral, antiproliferative, anti-inflammatory, and neuroprotective activities, making it a valuable tool for research in pain management and related therapeutic areas. -
μ-Opioid Receptor Agonist
Perillyl acetate is a monoterpene that acts as an agonist at the μ-opioid receptor. It demonstrates significant analgesic properties, making it valuable for studying pain management. This compound is also relevant in research related to inflammation and neurological conditions such as arthritis.
