Catalog No.
Product Name
Application
Product Information
Citations
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Deuterated Nepafenac
Nepafenac-d5 is a deuterated derivative of Nepafenac, a nonsteroidal anti-inflammatory drug that functions primarily as a topical COX-2 inhibitor with an IC50 of 0.12 μM. This compound exhibits minimal COX-1 inhibition (IC50 = 64.3 μM) and possesses prodrug characteristics, allowing it to rapidly convert to the active metabolite Amfenac in ocular tissues. Nepafenac-d5 is employed in research to investigate its efficacy in reducing inflammation and managing pain following ophthalmic procedures, as well as its potential to inhibit uveal melanoma metastasis in preclinical models. -
CRTh2 Antagonist
ARRY-502 is a potent and selective antagonist of the CRTh2 receptor, demonstrating oral bioavailability. By inhibiting PGD2-mediated Th2 inflammation, ARRY-502 effectively blocks eosinophil activation and airway hyperresponsiveness. This reagent holds significant potential for research applications focused on Th2-related asthma and related inflammatory disorders. -
Platelet Aggregation Inhibitor
17-Phenyl-18,19,20-trinor-PGD2 is a potent inhibitor of platelet aggregation that primarily targets adenosine diphosphate (ADP) signaling pathways. It demonstrates an IC50 of 8.4 μM, significantly outperforming prostaglandin D2 (PGD2), which has an IC50 of 18.6 nM. Additionally, 17-Phenyl-18,19,20-trinor-PGD2 serves as a weak agonist for cyclic AMP accumulation, making it a valuable tool for research in cardiovascular and hemostatic studies. -
CRTh2 Receptor Antagonist
NVP-QAV680 is a selective antagonist of the CRTh2 receptor, exhibiting low nanomolar potency in inhibiting CRTh2-mediated activation of human eosinophils and Th2 lymphocytes. This compound demonstrates significant oral bioavailability and has shown efficacy in models of CRTh2-dependent mechanisms and allergic diseases in rats. Its properties make NVP-QAV680 a valuable tool for research in allergy and immunology. -
Platelet Aggregation Inhibitor
Octimibate is a non-prostaglandin platelet aggregation inhibitor, acting primarily to prevent platelet activation and aggregation. This compound is utilized in research focused on cardiovascular diseases, specifically in the contexts of atherosclerosis and thrombosis, to elucidate the underlying mechanisms and potential therapeutic strategies for these conditions. -
Platelet Aggregation Inhibitor
MED 27 is a potent inhibitor of thromboxane synthase and thromboxane A2 receptors. It effectively inhibits rat platelet aggregation at significantly lower doses compared to acetylsalicylic acid. This compound is valuable for research applications focused on cardiovascular disorders and the mechanisms of platelet function. -
CRTH2 Antagonist
TASP0376377 is a highly potent and selective antagonist of the CRTH2 receptor, exhibiting an IC50 of 13 nM. This compound demonstrates strong binding affinity for CRTH2, with an IC50 of 19 nM. TASP0376377 is valuable for research applications focusing on inflammatory responses and immune modulation, particularly in studies related to asthma, allergy, and other CRTH2-related pathways. -
CRTH2 Antagonist
AM432 sodium is a selective antagonist of the CRTH2 receptor, also known as DP2. This compound exhibits high potency in human whole blood eosinophil assays, particularly under prolonged incubation conditions. Additionally, AM432 sodium has shown favorable pharmacokinetic profiles in canine and murine models of inflammatory diseases, making it a valuable tool for research in immunology and inflammatory pathways. -
Crth2 Antagonist
CRTh2 antagonist 3 is a potent antagonist of the chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2). This compound enhances the activity of phosphoinositide-dependent kinase-1 (PDK1) towards a short peptide substrate, exhibiting an EC50 of 2 μM and a Kd of 8.4 μM. Its potential applications include research into cardiovascular inflammation and the modulation of Th2-mediated responses. -
Ergot Derivatives
Cianergoline is an ergot derivative primarily known for its ability to reduce intraocular pressure (IOP). Its action is mediated by the inhibition of sympathetic nervous function through interactions with both prejunctional (DA2) and postjunctional (α1) adrenergic receptors. This compound is valuable for research applications focused on glaucoma and the underlying mechanisms of ocular hypertension. -
CRTh2 Antagonist
CRTh2 Antagonist 2 is a selective and potent CRTh2 receptor antagonist, exhibiting an IC50 of ≤10 nM. This compound is primarily utilized in research related to androgenic alopecia, offering valuable insights into the modulation of hair growth and related pathways. Its high specificity makes it an essential tool for investigating the therapeutic potential in hair loss disorders. -
Platelet Aggregation Inhibitor
CRL42872 free base is a potent oral platelet aggregation inhibitor that targets the mechanisms involved in platelet activation and aggregation. It effectively modulates platelet function, making it valuable for studying various cardiovascular and thrombotic disorders. Researchers can utilize CRL42872 free base to explore its potential therapeutic applications and elucidate the role of platelet aggregation in disease mechanisms. -
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. -
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
BPR1M97 is a dual-acting agonist for the mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor, exhibiting Ki values of 1.8 nM and 4.2 nM, respectively. This compound demonstrates significant potency and effective penetration of the blood-brain barrier, resulting in pronounced antinociceptive effects. BPR1M97 serves as a useful tool for research in pain management and opioid receptor biology. -
κ-opioid agonists
ICI-204448 is a κ-opioid receptor agonist that demonstrates limited central nervous system penetration. This compound effectively displaces the binding of the κ-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes. It is valuable for research applications focused on the role of κ-opioid receptors in pain modulation and neuropharmacology studies. -
μ Opioid Receptor Agonist
Loperamide is a selective μ opioid receptor agonist with Ki values of 3, 48, and 1156 nM for μ, δ, and κ opioid receptors, respectively. It demonstrates significant antinociceptive and antihyperalgesic properties, along with peripheral selectivity that enhances fluid, electrolyte, and glucose absorption. Loperamide effectively mitigates intestinal secretion induced by PGE2 and cholera toxin while reducing intestinal motility. This compound is applicable in research focused on inflammatory pain and chronic diarrhea. -
δ-opioid Agonist
KNT-127 is a selective δ-opioid receptor (DOR) agonist that effectively crosses the blood-brain barrier (Ki = 0.16 nM). It demonstrates high selectivity for the δ receptor, with Ki values of 0.16 nM, 21.3 nM, and 153 nM for δ, μ, and κ receptors, respectively. As a biased ligand, KNT-127 primarily activates cyclic adenosine monophosphate (cAMP) signaling while exhibiting lower beta-arrestin signaling. This compound enhances the release of dopamine and L-glutamate in key brain regions, including the striatum, nucleus accumbens, and prefrontal cortex, and is relevant for studies on neurological diseases due to its antidepressant and anxiolytic-like effects. -
Kappa Opioid Receptor Agonist
Anrikefon acetate is an agonist of the kappa opioid receptor, demonstrating notable analgesic activity. This compound is of interest in researching pain management and the modulation of mood disorders. Its selective action on kappa receptors makes it a valuable tool for investigating pathways involved in opioid receptor signaling and potential therapeutic applications. -
Opioid Receptor Agonist
[D-Ala2]leucine-enkephalin is a delta opioid receptor agonist designed for investigating opioid signaling pathways. This stable analog of Leu-enkephalin exhibits prolonged biological activity, making it a valuable tool for researchers studying the pharmacological effects and physiological roles of delta opioid receptors in various biological systems. Its resistance to enzymatic degradation allows for extended experiments without loss of efficacy. -
κ-opioid Receptor Agonist
Spiradoline mesylate is a selective kappa-opioid receptor (KOR) agonist with a Ki of 8.6 nM, demonstrating strong receptor affinity. It exhibits significant diuretic, analgesic, antiarrhythmic, antitussive, and neuroprotective activities, allowing it to effectively penetrate the blood-brain barrier. This compound is valuable for research applications focusing on pain management, addiction studies, and neuroprotection related to opioid activity. -
Opioid Receptor Modulator
Mitragynine pseudoindoxyl functions primarily as a μ-opioid receptor agonist with a Ki of 0.8 nM, while also acting as an antagonist at the δ-opioid receptor (Ki=3.0 nM). This compound exhibits moderate affinity for the κ-opioid receptor (Ki=24 nM) and operates through G protein-mediated signaling without β-arrestin-2 recruitment. Characterized by significant analgesic effects via a mixed μ-agonist/δ-antagonist mechanism, Mitragynine pseudoindoxyl demonstrates a reduced risk of common opioid side effects such as respiratory depression and dependency. Its potential applications include the management of hyperactivity and gastrointestinal transit inhibition, making it a candidate for therapeutic pain relief. -
Opioid Receptor Antagonist
Axelopran sulfate is a potent opioid receptor antagonist, exhibiting pKi values of 9.8, 8.8, and 9.9 for human recombinant μ and δ opioid receptors, as well as the guinea pig κ receptor. This compound is valuable for research focused on opioid signaling mechanisms and may aid in the investigation of pain management and addiction pathways. Its activity makes it a useful tool for elucidating the role of opioid receptors in various biological processes. -
Opioid Receptor Antagonist
LY255582 is a pan-opioid receptor antagonist, exhibiting high affinity for mu, delta, and kappa opioid receptors (Ki values of 0.4 nM, 5.2 nM, and 2.0 nM, respectively). This compound has been shown to reduce food intake and body weight, making it a valuable tool in obesity research. Its role in modulating opioid receptor activity offers potential insights into the mechanisms underlying appetite regulation and weight management. -
μ Opioid Receptor Modulator
BMS-986121 is a positive allosteric modulator of the μ opioid receptor, derived from innovative chemical scaffolds that represent a novel chemotype for this receptor. This compound enhances receptor activity and has potential applications in pain management research and the development of alternative analgesics. BMS-986121 is valuable for studies focused on the modulation of mu opioid receptor signaling pathways. -
Opioid Receptor Ligand
R-6890 is an opioid receptor ligand that acts as a selective antagonist, displaying significant binding affinity to rat opioid receptors with an IC50 of 4.6 nM in Tris buffer at pH 7.4. Its ability to displace radiolabeled opioids from receptors is notable, although its binding affinity is influenced by environmental conditions, particularly sodium chloride concentrations. R-6890 effectively crosses the blood-brain barrier and demonstrates analgesic properties in the warm water-induced tail-flick reflex assay in male Wistar rats, making it a valuable tool for research into pain mechanisms and opioid pharmacology. -
Opioid Receptor Agonist
Gluten Exorphin B5 is an opioid receptor agonist derived from wheat gluten. This peptide exhibits significant biological activity by enhancing postprandial plasma insulin levels in rodent models. It is used in research to investigate the role of opioid systems in metabolic processes and their potential implications for insulin regulation. -
κ-Opioid Receptor Antagonist
DIPPA hydrochloride is a selective, irreversible antagonist of the κ-opioid receptor, known for its high affinity and long-lasting effects. This compound demonstrates significant potential in research focused on anxiety and depression, facilitating investigations into its underlying mechanisms and therapeutic applications. Its unique pharmacological profile makes DIPPA hydrochloride a valuable tool for exploring the role of κ-opioid receptors in various neuropsychiatric conditions. -
δ-Opioid Receptor Agonist
Dalargin is a potent δ-opioid receptor agonist that exhibits significant biological activities, including nephroprotection. It mitigates cell death induced by gentamicin, thereby demonstrating protective effects against gentamicin-induced kidney injury. Additionally, Dalargin has shown antiulcer activity, making it a valuable compound for research applications in nephrology and gastrointestinal studies. -
Opioid Receptor Antagonist
Alvimopan metabolite hydrochloride is a peripherally selective opioid receptor antagonist that effectively reduces the amplitude of electrically induced contractions and spontaneous mechanical activity in guinea pig ileum. This compound is valuable for research applications investigating gastrointestinal motility and the pharmacological modulation of opioid receptors. Its ability to specifically target peripheral opioid receptors makes it a useful tool in studies related to pain management and gastrointestinal function. -
δ-Opioid Receptor Agonist
Deltorphin 2 is a selective agonist of the δ-opioid receptor, known for its potent biological activity in modulating pain and sensory perception. Its mechanism of action involves the activation of δ-opioid receptors, leading to analgesic effects. This compound is widely utilized in research applications focusing on pain management, neurobiology, and the exploration of opioid receptor signaling pathways.
