Catalog No.
Product Name
Application
Product Information
Citations
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PAR2 Antagonist
ENMD-1068 hydrobromide is a potent antagonist of the proteinase-activated receptor 2 (PAR2). It effectively attenuates joint inflammation in a dose-dependent manner, making it a valuable tool for investigating inflammatory pathways. This compound is primarily utilized in research related to joint inflammation and therapeutic approaches targeting PAR2. -
PAR4 Antagonist
P4pal10 is a potent antagonist of the protease-activated receptor 4 (PAR4). It effectively inhibits platelet aggregation and tissue factor (TF)-induced thrombin generation, exhibiting significant anticoagulant and antithrombotic properties. Additionally, P4pal10 reduces carrageenan-induced edema and granulocyte infiltration, and demonstrates protective effects in murine models of myocardial ischemia/reperfusion injury. This compound is valuable for research applications focused on thrombotic disorders and cardiovascular protection. -
PAR-1 Agonist
Parstatin (human) is a potent agonist of the protease-activated receptor 1 (PAR-1), derived from a thrombin receptor peptide. This cell-penetrating compound exhibits significant inhibition of angiogenesis, making it valuable for research into vascular biology and related diseases. Its ability to modulate PAR-1 activity has implications for studies focused on thrombosis, inflammation, and cancer. -
PAR1 Allosteric Inhibitor
ML161 analog 1 is a selective allosteric inhibitor targeting Proteinase-Activated Receptor 1 (PAR1) with an IC50 of 1.68 μM. This compound modulates PAR1 activity, making it a valuable tool for studying its role in various biological processes and disease mechanisms. Its application in research may provide insights into therapeutic strategies involving PAR1. -
PAR4 Agonist
PAR 4 (1-6) is a hexapeptide that acts as a specific agonist for protease-activated receptor 4 (PAR4). This bioactive compound plays a crucial role in signaling pathways associated with platelet activation and inflammatory responses. Researchers can utilize PAR 4 (1-6) in studies investigating cardiovascular health, hemostasis, and other PAR4-related biological processes. -
PAR-1 Agonist
TRAP-6 amide TFA is a potent agonist of the protease-activated receptor-1 (PAR-1). This peptide activates PAR-1 in response to thrombin, playing a critical role in mediating platelet activation and vascular responses. TRAP-6 amide TFA is commonly used in research applications focused on coagulation, cardiovascular biology, and the study of hemostatic mechanisms. -
Collagen/TRAP-6 Inhibitor
TRAP-6-IN-1 is a dual inhibitor targeting collagen and TRAP-6, with IC50 values of 17.12 µM and 11.88 µM, respectively. This compound effectively inhibits agonist-induced platelet aggregation in a non-competitive manner, making it a valuable tool for research into platelet function and coagulation disorders. Its dual action may provide insights into therapeutic strategies for cardiovascular diseases associated with platelet hyperactivity. -
PAR Agonist
SLIGRL-NH2 TFA is a potent agonist of Protease-Activated Receptor-2 (PAR-2). It is a peptide that specifically activates PAR-2, facilitating the study of its role in various physiological processes such as inflammation and pain modulation. This reagent is valuable for researchers exploring PAR-2 signaling pathways and their implications in disease mechanisms. -
PAR4 Antagonist
VU0652925 is a potent PAR4 antagonist, demonstrating IC50 values of 43 pM and 39.2 pM for PAC1 and P-selectin, respectively. This compound effectively inhibits GPIIbIIIa activation, making it a valuable tool for investigating the role of PAR4 in platelet activation and related cardiovascular research applications. -
PAR-2 Inhibitor
PAR-2-IN-2 is a selective inhibitor of protease-activated receptor 2 (PAR-2), exhibiting an IC50 of 10.79 μM against the PAR-2 peptide SLIGKV, while demonstrating a significantly higher IC50 of over 200 μM for Trypsin. This compound is valuable for studying PAR-2 signaling pathways and exploring its role in inflammatory responses and pain modulation. PAR-2-IN-2 serves as a critical tool for researchers investigating therapeutic targets in conditions associated with PAR-2 activation. -
NPY Y1/NPFF Receptor Antagonist
BIBP3226 is a selective antagonist of the neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptors, exhibiting K_i values of 1.1 nM, 79 nM, and 108 nM for rat NPY Y1, human NPFF2, and rat NPFF, respectively. This compound has demonstrated anxiogenic-like effects, making it a valuable tool for research in neuropharmacology, particularly in studies exploring anxiety-related disorders and the modulation of neuropeptide signaling pathways. -
NPY Y5 antagonist
S 25585 is a selective antagonist of the neuropeptide Y (NPY) Y5 receptor. This compound is primarily utilized in research focused on appetite regulation, demonstrating a significant ability to reduce food intake without directly blocking the Y5 receptor. Its unique mechanism makes it an essential tool for studying the intricate pathways involved in energy homeostasis and metabolic disorders. -
NPY-5 Receptor Antagonist
Neuropeptide Y5 receptor ligand-1 is a potent antagonist of the neuropeptide Y5 (NPY-5) receptor. This carbazole derivative is utilized in research applications focused on the role of NPY-5 in various physiological processes, including regulation of appetite, anxiety, and circadian rhythms. By inhibiting NPY-5 receptor activity, it provides valuable insights into neuropeptide signaling pathways and their implications in metabolic and neurobehavioral disorders. -
NPY-5 Receptor Antagonist
NPY-5 receptor antagonist-1 is a potent antagonist of the neuropeptide Y5 (NPY-5) receptor, exhibiting a Ki value of less than 1 μM. This compound is invaluable for investigating the roles of NPY-5 in obesity, feeding disorders, and various neurological conditions. Its ability to modulate NPY-5 receptor activity makes it a useful tool in pharmacological research and drug development related to metabolic and neuropsychiatric disorders. -
NPY Y5 Receptor Agonist
(D-Trp32)-Neuropeptide Y (porcine) is a selective agonist of the neuropeptide Y (NPY) Y5 receptor. It exhibits orexigenic activity, thereby promoting increased food intake, and has been shown to inhibit Forskolin-stimulated cAMP formation. This peptide is valuable for research focusing on appetite regulation and metabolic disorders. -
NPY Y1 Receptor Antagonist
BVD 10 is a highly selective antagonist of the neuropeptide Y (NPY) Y1 receptor. This compound effectively inhibits NPY-induced increases in glutamate levels, providing insights into neurochemical interactions. BVD 10 is particularly valuable for research focused on seizure mechanisms and related neurological studies. -
NPY Receptor Antagonist
BIIE-0246 dihydrochloride is a potent and highly selective non-peptide antagonist of the neuropeptide Y (NPY) Y2 receptor, exhibiting an IC50 value of 15 nM. This compound effectively inhibits NPY signaling, making it valuable for research on appetite regulation, neuroprotection, and anxiety-related disorders. BIIE-0246 dihydrochloride provides a robust tool for investigating the physiological roles of NPY and its involvement in various pathophysiological conditions. -
NPY Y2Antagonist
NPY Y2 Antagonist 2 is a selective inhibitor of the neuropeptide Y receptor Y2, exhibiting pKi values of 6.8 nM and 7.2 nM in human and rat brain tissues, respectively. This compound effectively blocks the NPY Y2-mediated negative feedback, leading to increased endogenous NPY release and enhanced activation of Y1 receptors. Its ability to penetrate the blood-brain barrier, along with moderate in vivo clearance and a favorable brain/plasma ratio, makes NPY Y2 Antagonist 2 a valuable tool for investigating mood disorders, alcohol withdrawal-related anxiety, and social anxiety linked to nicotine withdrawal. -
Neuropeptide FF Receptor Agonist
Neuropeptide SF (mouse, rat) is a potent agonist of the neuropeptide FF receptors, exhibiting Ki values of 48.4 nM for NPFF1 and 12.1 nM for NPFF2. This compound enhances the sustained current of heterologously expressed acid-sensing ion channel 3 (ASIC3), making it a valuable tool in studies related to pain modulation and neuropeptide signaling. Neuropeptide SF is ideal for research investigating neurophysiological processes and receptor interactions within neural pathways. -
NPY5 Receptor Antagonist
SCH 430765 is a potent and selective antagonist of the neuropeptide Y5 (NPY5) receptor. This compound plays a significant role in modulating appetite and energy homeostasis, making it valuable for research into obesity and related metabolic disorders. Its ability to inhibit NPY5 receptor activity provides insights into potential therapeutic strategies for weight management and obesity-related conditions. -
NPY Y2 Antagonist
NPY Y2 Antagonist 1 is a selective antagonist of the neuropeptide Y receptor Y2 (NPY Y2), primarily functioning through competitive inhibition. This compound exhibits significant biological activity in modulating neuropeptide Y signaling pathways, making it invaluable for research focused on neurobiology and related therapeutic areas. Its application extends to studying the physiological roles of NPY receptors in various biological processes and potential implications in metabolic disorders and appetite regulation. -
Neurotensin Receptor Activator
[Lys8, Lys9]-Neurotensin (8-13) is a neurotensin analog that primarily activates the G protein-coupled receptors NTS1 and NTS2. This compound demonstrates potent analgesic activity, with binding affinities (Ki values) of 0.33 nM and 0.95 nM for the human NTS1 and NTS2 receptors, respectively. It is utilized in research applications investigating pain modulation and neuropeptide signaling pathways. -
Neurotensin Receptor Agonist
JMV 449 acetate is a highly potent agonist of the neurotensin receptor. It demonstrates an IC50 of 0.15 nM in inhibiting 125I-neurotensin binding to neonatal mouse brain tissue and an EC50 of 1.9 nM in inducing contractions in the guinea-pig ileum. Additionally, JMV 449 acetate exhibits significant, long-lasting hypothermic and analgesic effects in mouse models, making it valuable for research in pain management and neuropharmacology. -
Neurotensin Octapeptide
Xenopsin is a neurotensin-like octapeptide derived from the skin of Xenopus laevis. It primarily functions as an inhibitor of Tetragastrin-stimulated gastric acid secretion, making it valuable for studies related to gastrointestinal physiology and acid regulation. Research applications include investigations into peptide signaling pathways and gastrointestinal disorders. -
Neurotensin Analog
Acetyl neurotensin (8-13) is a neurotensin analog that retains full binding affinity and pharmacological activity. This compound is primarily utilized in research exploring neurotensin receptor interactions and their implications in various physiological processes. Its use may aid in the investigation of neuroinflammatory conditions, pain modulation, and appetite regulation. -
Neurotensin Receptor Inhibitor
VGD071 is a neurotensin receptor inhibitor that specifically targets sortilin. This compound exhibits potential for modulating neurotensin signaling pathways, which may be relevant in the context of breast cancer research. VGD071 is suitable for preclinical studies and investigations into the role of neurotensin receptors in tumorigenesis and cancer progression. -
Neurotensin Receptor Modulator
[D-Trp11]-Neurotensin is a neurotensin receptor modulator that acts as a selective antagonist in perfused rat hearts while exhibiting full agonistic activity in guinea pig atria and rat stomach strips. This compound has demonstrated the ability to inhibit neurotensin-induced hypotension, making it a valuable tool for studying neurotensin receptor dynamics and their physiological effects. Its diverse biological activity supports various research applications, including cardiovascular and gastrointestinal studies. -
Neurotensin Receptor Agonist
Neurotensin(8-13) TFA is an active fragment of the neuropeptide neurotensin, specifically acting as an agonist of neurotensin receptors. This compound has been shown to decrease the density of cell-surface NT1 receptors (NTR1), impacting various signaling pathways. It is useful in research applications focused on neurobiology, pharmacology, and the study of neurotensin-related pathways in health and disease. -
Neurotensin Receptor Agonist
Contulakin G is an O-glycosylated neurotensin analog that functions as an agonist of the neurotensin receptor. This compound exhibits notable antinociceptive properties, making it valuable in pain modulation research. Its unique characteristics allow for exploration in neurobiology and potential therapeutic applications targeting pain relief mechanisms. -
Neurotensin Receptor
SR 142948-C3-NHMe is a selective antagonist of the neurotensin receptor. This compound has demonstrated significant inhibitory activity against neurotensin signaling pathways, making it a valuable tool for studying neurotensin-related physiological processes. It is applicable in research focused on neuropharmacology, pain modulation, and various CNS disorders, providing insight into neurotensin's role in these conditions. -
Neurotensin Receptor Agonist
JMV 449 is a potent neurotensin receptor agonist, demonstrating an IC50 of 0.15 nM for the inhibition of [125I]-neurotensin binding in neonatal mouse brain assays. Additionally, it shows an EC50 of 1.9 nM in inducing contractions in the guinea pig ileum. JMV 449 exhibits significant hypothermic and analgesic effects in murine models, making it a valuable tool for research in pain management and neuropharmacology. -
Neurotensin Inhibitor
L-156903 is a potent neurotensin inhibitor that selectively disrupts the binding of neurotensin to brain tissue. This compound is valuable for studying the neurotensinergic system and its role in various neurological conditions. Its inhibitory action can contribute to research aimed at understanding the mechanisms underlying neuropsychiatric disorders and potential therapeutic interventions. -
Opioid Receptor Agonist
CCI-1008 is an opioid receptor agonist that exhibits significant activity in targeting the µ-opioid receptor. It is primarily utilized in research related to nervous system diseases, exploring mechanisms of pain modulation and addiction. This compound serves as a valuable tool for investigating therapeutic strategies aimed at managing pain and opioid-related disorders. -
κ Opioid Receptor Antagonist
Norbinaltorphimine dihydrochloride selectively antagonizes the κ-opioid receptor, making it an important tool for research on opioid signaling pathways. Its potent inhibitory action allows for the investigation of κ-opioid receptor-related biological processes and potential therapeutic applications in pain management and addiction studies. Researchers can utilize this compound to explore the effects of opioid receptor modulation in various experimental settings. -
Opioid receptor Antagonist
Naloxone is an antagonist of opioid receptors, primarily acting to reverse the effects of opioid overdose. It effectively alleviates respiratory depression caused by opioid toxicity, restoring normal breathing. Research applications include studies on opioid overdose treatment, respiratory pharmacodynamics, and the examination of opioid receptor interactions. Naloxone may also induce pulmonary edema and cardiac arrhythmias as potential side effects. -
Opioid Receptor Antagonist
Naltrexone is a long-acting antagonist of opioid receptors, including μ, κ, and δ subtypes. It effectively blocks the euphoric effects of exogenous opioids and diminishes alcohol cravings by antagonizing these receptors. Clinically, low doses of Naltrexone are utilized for chronic pain management, the treatment of inflammatory conditions, and potentially inhibiting tumor growth. Additionally, it is employed to alleviate intractable pruritus associated with psoriasis and atopic dermatitis, while its combination with Bupropion may contribute to reduced food cravings and body weight management. -
δ-opioid Receptor Agonist
SNC80 is a highly selective and potent non-peptide δ-opioid receptor agonist, demonstrating a Ki of 1.78 nM and an IC50 of 2.73 nM. This compound selectively activates the μ-δ heteromer in HEK293 cells, exhibiting an EC50 of 52.8 nM. SNC80 is characterized by its antinociceptive, antihyperalgesic, and antidepressant-like activities, making it a valuable tool for research in the treatment of various headache disorders. -
DOR Agonist
DPDPE is a selective δ-opioid receptor (DOR) agonist known for its anticonvulsant properties. This opioid peptide is utilized in research to explore its potential therapeutic effects in pain management and seizure disorders. Its specificity for DORs makes DPDPE a valuable tool for investigating opioid receptor signaling pathways and their implications in neurological studies. -
μ-Opioid Receptor Agonist
Endomorphin 1 is a selective agonist of the μ-opioid receptor, exhibiting a high affinity with a Ki value of 1.11 nM. It also shows moderate affinities for kappa3 binding sites, with Ki values ranging from 20 to 30 nM. This compound is known for its antinociceptive properties, making it relevant for research focused on pain modulation and opioid receptor signaling pathways. -
μ-opioid Receptor Antagonist
Naldemedine tosylate is a selective μ-opioid receptor antagonist, classified as a peripherally acting mu-opioid receptor antagonist (PAMORA). It exhibits high binding affinities for human μ-, δ-, and κ-opioid receptors, making it a valuable reagent for studying opioid-related pathways. Its primary application includes research on opioid-induced constipation (OIC). Additionally, Naldemedine tosylate has the potential to interact with the 3CLpro protease encoded by the SARS-CoV2 genome, suggesting further avenues for investigation in viral studies. -
Kappa-opioid Receptor Antagonist
Nor-Binaltorphimine is a selective antagonist of the kappa-opioid receptor, known for its role in modulating nociception and mood regulation. This compound exhibits prolonged effects in vivo, making it a valuable tool in research related to pain management, addiction, and psychiatric disorders. Its specificity for kappa-opioid receptors supports studies focused on understanding their physiological and pathological roles. -
KOR Agonist
(-)-U-50488 hydrochloride is a selective agonist of the kappa-opioid receptor (KOR), exhibiting a binding affinity (Kd) of 2.2 nM, significantly higher than its affinity for the μ-opioid receptor (MOR) at 430 nM. This compound serves as a more active enantiomer compared to its (+) counterpart and the racemic mixture. In research applications, (-)-U-50488 hydrochloride demonstrates potent and sustained anti-HIV activity in infected blood monocyte-derived macrophages (MDM), making it a valuable tool for studying kappa-opioid receptor functions and their therapeutic potential in HIV-related research. -
µ-Opioid Receptor Positive Allosteric Modulator
BMS-986122 is a selective positive allosteric modulator of the mu-opioid receptor (µ-OR) that enhances the activity of orthosteric agonists. This compound effectively increases β-arrestin recruitment, inhibits adenylyl cyclase, and activates G protein signaling pathways. BMS-986122 demonstrates the ability to potentiate DAMGO-mediated [35S]GTPγS binding in mouse brain membranes, making it a valuable tool for research in pain management and opioid pharmacology. -
Opioid Receptor Agonist
BW-180C, a δ opioid receptor (DOR) agonist, is a member of the enkephalin family. This compound exhibits neuroprotective properties and reversibly inhibits cellular transcription in neurons while preserving cell integrity. BW-180C is valuable for research applications focused on neuroprotection and opioid receptor signaling. -
Kappa Receptor Ligand
Dynorphin A (1-8) is a potent kappa receptor ligand, playing a critical role in opioid signaling. This peptide exhibits significant binding affinity, inhibiting the binding of 3H-Bremazocine to the purified kappa receptor with an IC50 of 303 nM. It serves as a valuable tool for studying kappa opiate pharmacology and exploring its implications in pain modulation and neurobiology. -
Opioid Receptor Antagonist
Naloxone methiodide is a peripherally restricted, nonselective competitive antagonist of opioid receptors. Its lack of ability to penetrate the blood-brain barrier allows for targeted effects in peripheral tissues. This compound is primarily used in research applications investigating opioid receptor activity and the modulation of peripheral opioid effects, making it valuable for studying pain management and opioid-related responses. -
ORL1 Receptor Antagonist
(±)-J-113397 is a selective non-peptidyl antagonist of the ORL1 receptor, exhibiting a Ki value of 1.8 nM for cloned human ORL1. It effectively inhibits nociceptin/orphanin FQ-stimulated GTPγS binding in CHO cells expressing ORL1, with an IC50 of 5.3 nM. This compound is valuable for investigating the physiological roles and functions of the nociceptin/orphanin FQ system in various biological contexts. -
δ-opioid Receptor Agonist
SNC162 is a potent δ-opioid receptor agonist with an IC50 of 0.94 nM. This compound demonstrates significant antidepressant-like and antinociceptive properties, making it a valuable tool in the investigation of pain management and mood disorders. Its efficacy in modulating δ-opioid receptor activity supports research into therapeutic applications for treatment-resistant depression and chronic pain syndromes. -
KOR Agonist
(±)-U-50488 hydrochloride is a selective agonist of the κ opioid receptor (KOR). It exhibits significant analgesic and anti-inflammatory properties, making it valuable for studies related to pain management and opioid receptor signaling pathways. This compound is ideal for research applications investigating the role of KOR in various physiological processes and potential therapeutic interventions. -
δ-opioid Receptor Antagonist
TAN-452 is a selective, orally active δ-opioid receptor antagonist, exhibiting a Ki of 0.47 nM and a Kb of 0.21 nM. This reagent also shows antagonistic properties toward μ-opioid receptors, with a Ki of 36.56 nM, and κ-opioid receptors, with a Ki of 5.31 nM. TAN-452 is designed to attenuate morphine-induced side effects while maintaining analgesic efficacy, making it valuable for research in pain management and opioid-related studies. Its low brain penetrability further supports peripheral applications, minimizing central nervous system interactions.
