Catalog No.
Product Name
Application
Product Information
Citations
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mGluR1 antagonist
(RS)-4C3HPG, or 4-Carboxy-3-hydroxyphenylglycine, serves as a competitive antagonist of the metabotropic glutamate receptor 1 (mGluR1) in the central nervous system and acts as an agonist at mGluR2/3. This compound demonstrates neuroprotective properties in models of acute global ischemia, making it a valuable tool for investigating glutamate receptor signaling and associated neuroprotective mechanisms. Its dual activity presents opportunities for research in neurodegenerative diseases and synaptic modulation. -
Motilin Receptor Antagonist
MA-2029 is a selective, orally active antagonist of the motilin receptor, exhibiting an IC50 of 4.9 nM. It demonstrates high selectivity for the motilin receptor compared to a variety of other receptors and ion channels. This compound is particularly relevant for research into gastrointestinal disorders linked to impaired gastrointestinal motility, providing a valuable tool for studying motility-related pathophysiology and potential therapeutic interventions. -
Motilin Receptor Agonist
Motilin (26-47), human, porcine is a potent agonist of the motilin receptor, exhibiting a Ki value of 2.3 nM and an EC50 of 0.3 nM in a Chinese hamster ovary cell line. This peptide plays a critical role in gastrointestinal motility and is instrumental in research focused on digestive system disorders and hormone signaling pathways. Its application extends to various studies involving gut motility regulation and the therapeutic potential of motilin-related compounds. -
Smooth Muscle Contraction Agonist
Motilin, canine is a 22-amino acid peptide that acts as a potent agonist of gastrointestinal smooth muscle contraction. This bioactive peptide plays a crucial role in stimulating intestinal motility and has potential applications in gastrointestinal research. It is primarily used to study motility disorders and the regulation of digestive processes in canine models. -
Motilin Agonist
KC-11458 is a motilin agonist that enhances gastric motility by stimulating motilin receptors in the gastrointestinal tract. This compound is primarily used for research into gastrointestinal motility disorders and can be valuable in studies investigating the regulation of gastric emptying processes. Its ability to accelerate gastric emptying makes it a potential tool for exploring therapeutic targets in digestive disorders. -
Motilin Agonist
EM-523 is a motilin agonist and an erythromycin derivative that selectively targets motilin receptors. It has demonstrated biological activity with pED50 values of 8.19 and 6.08 for inducing contractions in rabbit small intestinal tissue and human duodenal tissue, respectively. This compound is valuable for investigating gastrointestinal diseases and advancing research related to motility disorders. -
Motilin Analogue
[Leu13]-Motilin is a motilin analogue that primarily targets motilin receptors. This compound promotes gastrointestinal motility by inducing concentration-dependent contractions in various segments of the gastrointestinal tract, including the gastric antrum, duodenum, jejunum, ileum, and descending colon. [Leu13]-Motilin is utilized in research to explore the mechanisms of gut motility and to investigate potential therapeutic applications in gastrointestinal disorders. -
Motilin Antagonist
ANQ-11125 is a potent and selective antagonist of motilin, exhibiting a pKd of 8.24. This compound effectively inhibits motilide-induced contractions in vitro in rabbit models, making it a valuable tool for studying gastrointestinal motility and related disorders. ANQ-11125 has potential applications in research focused on gastrointestinal physiology and pharmacology. -
Gastrointestinal Hormone
Motilin, human, porcine, is a gastrointestinal hormone that plays a critical role in regulating gastrointestinal motility. Released during fasting, eating, and water intake, Motilin enhances enteric cholinergic activity in the human stomach with an EC50 of 33 nM. This biological activity makes it a valuable tool for research into gastrointestinal function and motility disorders. -
Motilin Receptor Agonist
Mitemcinal fumarate is a selective agonist of the motilin receptor. It demonstrates significant biological activity in promoting defecation and increasing stool bulk without causing excessive diarrhea, as evidenced in preclinical studies in rabbits and dogs. Its rapid onset and short duration of action suggest potential applications in the treatment of constipation, making it a valuable compound for gastrointestinal research. -
Motilin receptor agonist
Mitemcinal is an oral motilin receptor agonist, specifically targeting motilin pathways to enhance gastrointestinal motility. Research demonstrates its capability to promote defecation in animal models, such as rabbits and dogs, without inducing severe diarrhea. Additionally, Mitemcinal increases stool weight while maintaining water content and reduces the latency to first defecation in dogs. This makes Mitemcinal a promising candidate for studies on constipation management and gastrointestinal disorders. -
Motilin Receptor Agonist
EM574 is a potent agonist of the motilin receptor, demonstrating significant activity in the human gastric antrum and rabbit gastrointestinal tract in vitro. As an erythromycin derivative, EM574 is utilized in research applications exploring gastrointestinal motility and related disorders. Its ability to selectively modulate motilin receptor signaling makes it a valuable tool for advancing studies in gastrointestinal physiology and pharmacology. -
Motilin Receptor Agonist
[Nle13]-Motilin is a synthetic analog of motilin that functions as a motilin receptor agonist. It effectively stimulates gastrointestinal motility by activating the motilin receptor, making it a valuable tool in studies related to gastrointestinal physiology and potential therapeutics for gut motility disorders. Research applications include investigations into the modulation of gastric emptying and the treatment of gastrointestinal dysmotility. -
Motilin Receptor Agonist
Atilmotin is a selective motilin receptor agonist with a pKd value of 8.94. It enhances gastrointestinal motility by increasing lower esophageal sphincter (LES) and gastric pressures, making it a valuable tool for studying esophageal and gastric motility. This compound is particularly relevant for research applications focused on gastrointestinal disorders and the development of prokinetic agents. -
Motilin Receptor Antagonist
RWJ-68022 is a cyclopentene derivative that acts as a motilin receptor antagonist. It effectively competes with motilin and erythromycin for binding to the motilin receptor site. This compound is valuable in research related to gastrointestinal disorders, providing insights into motilin's role in digestive physiology and its potential therapeutic applications. -
NPR3 Antagonist
AP 811 is a selective antagonist of the natriuretic peptide clearance receptor (NPR3) with a binding affinity (Ki) of 0.48 nM. It demonstrates over 20,000-fold selectivity for NPR3 compared to NPR1. AP 811 effectively inhibits atrial natriuretic peptide (ANP)-induced stimulation of transport pumps, making it a valuable tool for research into cardiovascular and kidney function regulation. -
ANP antagonist
A 71915 is a potent and competitive antagonist of the natriuretic peptide receptor A (NPRA), exhibiting a pKi value of 9.18. It effectively displaces [125I]ANP in a dose-dependent manner, with a dissociation constant (Ki) of 0.65 nM. In cellular assays, A 71915 demonstrates a significant inhibition of rat ANP-induced cGMP production in NB-OK-1 cells, making it a valuable tool for research into cardiovascular signaling pathways and related therapeutic applications. -
Npr1 Inhibitor
JS11 is a selective inhibitor of natriuretic polypeptide receptor 1 (Npr1), exhibiting an IC50 of 1.9 μM for human Npr1. This compound has demonstrated the ability to alleviate pruritus in mouse models, making it a valuable tool for investigating the role of Npr1 in pruritic conditions. Its pharmacological activity positions JS11 as a significant reagent for research in dermatology and other fields related to itch sensation and regulation. -
NPR-C Ligand
ANP [Des18-22] 4-23 amide (rat) is a polypeptide fragment derived from rat atrial natriuretic peptide (ANP) that selectively interacts with the natriuretic peptide receptor C (NPR-C). This compound is instrumental in studying NPR-C signaling pathways and evaluating the physiological effects of natriuretic peptides in cardiovascular research and related fields. Its specificity for NPR-C makes it a valuable tool for in vitro experiments aimed at elucidating receptor-mediated responses. -
Neuropeptide
BNP(1-32), porcine is an atrial natriuretic peptide that primarily targets neuropeptide pathways. This cardiac hormone exhibits significant natriuretic, diuretic, and vasorelaxant effects, making it valuable for cardiovascular research. Furthermore, BNP(1-32) has been shown to influence passive avoidance learning in rodent models, highlighting its potential role in neurobiology studies involving dopaminergic and cholinergic systems, as well as adrenergic receptor interactions. -
NPRA/NPR1 Agonist
NPRA agonist-11 is a selective agonist of the natriuretic peptide receptor A (NPRA/NPR1), exhibiting AC50 values of 1.681 μM in humans and 0.989 μM in monkeys. This compound is integral to studies of cardiovascular diseases and may also be applicable in the exploration of related disorders. Its mechanism of action makes it a valuable tool for researchers investigating NPRA signaling pathways and their implications in physiological and pathological contexts. -
Vasodilator
Ularitide, also known as Urodilatin, is a potent vasodilator that functions through the activation of renal receptors. This natriuretic peptide plays a critical role in the regulation of renal dopamine metabolism, contributing to its cardiovascular effects. Ularitide is widely used in research related to heart failure, providing insights into renal function and fluid balance in the context of cardiovascular health. -
NPRs Agonist
Nesiritide acetate is a recombinant human B-type natriuretic peptide that acts as an agonist of natriuretic peptide receptors (NPRs), exhibiting Kd values of 7.3 pM and 13 pM for NPR-A and NPR-C, respectively. This compound regulates the activation and inactivation of L-type calcium channels, demonstrating significant vasodilatory, diuretic, and natriuretic actions. It is primarily utilized in the research of cardiovascular conditions, particularly heart failure and vascular remodeling following arterial injury. -
Vasodilator
Atriopeptin III (rat), a 24-amino acid atrial peptide, serves as a potent vasodilator and natriuretic agent. This compound enhances renal function while effectively reducing blood pressure, particularly demonstrated in ureter-obstructed rat kidney models. Atriopeptin III (rat) is valuable for research related to chronic renal failure and its associated mechanisms. -
Diuretic
Ethiazide is a thiazide diuretic that functions by inhibiting renal reabsorption of sodium and water, leading to increased urine output. This compound is effective in reducing fluid retention, lowering blood volume, and consequently decreasing blood pressure. Ethiazide serves as a valuable tool in cardiovascular research, aiding investigations related to fluid balance and hypertension management. -
NK2R Agonist
EB1002 is a highly selective, long-acting agonist of the NK2 receptor (NK2R). This compound plays a crucial role in central appetite suppression, stimulates peripheral energy expenditure, and enhances insulin sensitivity, leading to effective reductions in body weight and improvements in glucose and lipid metabolism. EB1002 is a valuable tool for research focused on obesity and type 2 diabetes. -
Glutamate Derivative
H-Glu(OtBu)-OtBu hydrochloride is a glutamate derivative that serves as a critical intermediate in the synthesis of prostate-specific membrane antigen (PSMA) targeting probes. This compound enhances tumor/background contrast by utilizing negatively charged linkers to minimize nonspecific background binding. Its applications are primarily in prostate cancer PET and SPECT imaging studies, facilitating improved diagnostic imaging. -
NK-1/NK-3 Receptor Antagonist
Elinzanetant is an orally bioavailable and selective antagonist of the neurokinin-1 (NK-1) and neurokinin-3 (NK-3) receptors. It exhibits significant efficacy in alleviating menopause-associated vasomotor symptoms such as hot flashes and night sweats while also influencing levels of estradiol and progesterone. This compound is valuable for researching treatments for moderate to severe vasomotor and sleep disorders related to menopause. -
p75 Neurotrophin Receptor Ligand
LM11A-31 is a non-peptide ligand targeting the p75 neurotrophin receptor (p75NTR) and functions as a potent antagonist of proNGF (nerve growth factor). This orally active amino acid derivative demonstrates high permeability across the blood-brain barrier and effectively inhibits p75-mediated neurodegeneration. Research indicates that LM11A-31 can reverse cholinergic neurite dystrophy in mouse models of Alzheimer's disease, particularly during mid- to late-stage disease progression, making it valuable for studying neurodegenerative conditions and developing therapeutic strategies. -
NK1 Receptor Antagonist
L-733060 hydrochloride is a selective neurokinin-1 (NK-1) receptor antagonist that primarily targets pain transmission and neural plasticity. By inhibiting the binding of Substance P to the NK-1 receptor, L-733060 hydrochloride effectively blocks the enhancement of long-term potentiation (LTP) in the hippocampus. This compound has demonstrated the ability to reverse orofacial hyperalgesia induced by experimental occlusal interference in rat models. Additionally, L-733060 hydrochloride inhibits neurogenic plasma extravasation without adverse effects on cardiovascular function and may possess anti-tumor properties. It is suitable for exploring mechanisms of chronic orofacial pain. -
NK-1 Receptor Antagonist
L-732138 is a selective and potent antagonist of the neurokinin-1 (NK-1) receptor, exhibiting an IC50 of 2.3 nM. This compound demonstrates a 200-fold greater potency in cloned human NK-1 receptors compared to cloned rat NK-1 receptors, and is more than 1000-fold more selective than human NK-2 and NK-3 receptors. L-732138 is useful in research focused on pain modulation, particularly in the reduction of hyperalgesia, and has shown potential antitumor activity. -
Neurokinin Receptor Agonist
GR-73632 is a novel neurokinin 1 (NK-1) receptor agonist that directly targets the peripheral terminals of primary sensory neurons. By activating the NK-1 receptor, GR-73632 effectively conveys itch signals, making it a valuable tool in studying mechanisms of pruritus and related sensory pathways. This compound is relevant for research applications focusing on itch-related disorders and sensory neuron functionality. -
Neurotransmitter
Substance P TFA, a CNS-penetrant neuropeptide, primarily targets the neurokinin 1 receptor (NK1R). This compound functions as both a neurotransmitter and neuromodulator within the central nervous system, playing a crucial role in mediating pain perception, anxiety, and stress responses. Its application in research includes studying neuronal signaling pathways and exploring therapeutic approaches for pain management and psychiatric disorders. -
Neurokinin-1 Receptor Antagonist
Orvepitant maleate is a potent and selective antagonist of the neurokinin-1 (NK-1) receptor, exhibiting a pKi of 10.2 for the human receptor. This orally active compound effectively crosses the blood-brain barrier, making it a valuable tool in neurological research. Orvepitant maleate shows promise for therapeutic applications in depressive disorders and chronic refractory cough (CRC), providing insights into the modulation of neurokinin pathways. -
NK3 Receptor Antagonist
Osanetant is a selective antagonist of the neurokinin-3 (NK3) receptor. This compound exhibits anxiolytic and antidepressant-like effects, making it a valuable tool for research in the fields of anxiety, depression, and schizophrenia. Its mechanism of action involves modulation of neurokinin signaling pathways, providing insights into potential therapeutic applications for mood disorders. -
NK-1R Antagonist
Spantide II is a potent neurokinin-1 receptor (NK-1R) antagonist, functioning as an undecapeptide analog of substance P. By binding to NK-1R, Spantide II effectively inhibits the proinflammatory activities associated with substance P. This reagent is valuable for research into inflammatory skin disorders, including psoriasis and contact dermatitis, contributing to the understanding of neurogenic inflammation. -
Neurokinin Receptor Antagonist
Vapreotide is a neurokinin-1 (NK1) receptor antagonist, demonstrating an IC50 of 330 nM. It effectively inhibits the binding of substance P to the NK1 receptor, making it a valuable tool in research concerning pain modulation, anxiety, and the regulation of neurogenic inflammation. Vapreotide's applications extend to studies of gastrointestinal disorders and therapeutic strategies for conditions associated with elevated neurokinin levels. -
Neurokinin Receptor Modulator
Biotin-Substance P is a biotinylated form of the neuropeptide Substance P, which primarily targets the neurokinin 1 receptor (NK1R). This compound acts as both a neurotransmitter and neuromodulator within the central nervous system (CNS), playing a crucial role in pain perception, stress response, and neuroinflammation. Biotin-Substance P is particularly useful in research applications focused on neurokinin receptor signaling pathways and neuropeptide interactions in various physiological and pathological conditions. -
Neurokinin Receptor Activator
Eledoisin Related Peptide is a neurokinin receptor activator that functions as an analog of Substance P. This peptide is known to stimulate neurons, resulting in various behavioral responses. It serves as a valuable tool for research applications focused on neurokinin signaling pathways and tachykinin receptor interactions. -
Active Compound
Substance P (7-11) is a C-terminal fragment of the neuropeptide Substance P, primarily known for its role in modulating pain perception and inflammatory responses. This compound increases intracellular calcium concentrations, leading to diverse biological activities. It is widely utilized in research related to neurobiology, pain signaling pathways, and inflammation response mechanisms. -
Tachykinin NK1 Receptor Agonist
[Sar9,Met(O2)11]-Substance P is a selective agonist for the tachykinin NK1 receptor. It exhibits significant biological activity, promoting receptor activation which is implicated in pain modulation, stress response, and neurogenic inflammation. This compound is valuable for research applications in neurobiology, pain syndromes, and the study of substance P-related pathways. -
NK1 Receptor Antagonist
Spantide I is a selective antagonist of the neurokinin-1 (NK1) receptor, demonstrating Ki values of 230 nM for NK1 and 8150 nM for NK2 receptors. This compound effectively modulates cytokine profiles by reducing type 1 and enhancing type 2 cytokine IL-10 in the infected cornea, thereby significantly decreasing corneal perforation. Spantide I serves as a valuable tool in research focused on inflammatory responses and therapeutic interventions in corneal diseases. -
Neurokinin 1 Receptor Agonist
Hemokinin 1 (mouse) is a selective agonist of the neurokinin-1 receptor (NK1R), exhibiting a Ki value of 0.175 nM for mouse NK1R. This compound demonstrates a much lower affinity for the human NK2 receptor, with a Ki of 560 nM. Hemokinin 1 is primarily utilized in research applications aimed at studying pain modulation, inflammatory processes, and neurogenic signaling pathways involving the NK1 receptor. -
NK2R Agonist
[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) is a selective agonist of the NK2 receptor (NK2R) that demonstrates potent biological activity. This peptide analog of Neurokinin A exhibits prokinetic effects, making it valuable for research into gastrointestinal motility and related pathways. Its application can elucidate the role of NK2R in smooth muscle contraction across various tissues, providing insights into receptor functionality and potential therapeutic targets. -
NK1 Receptor Antagonist
Rolapitant hydrochloride hydrate is a potent and selective neurokinin 1 (NK1) receptor antagonist, exhibiting a Ki value of 0.66 nM. This compound is known for its long-acting and orally bioactive properties, making it suitable for therapeutic applications. Notably, Rolapitant hydrochloride hydrate demonstrates significant anti-emetic activity, as evidenced in ferret emesis models, supporting its potential use in managing nausea and vomiting. Additionally, it does not interact with CYP3A4, allowing for broader applicability in combination therapies. -
Neurokinin Receptor Antagonist
Vapreotide acetate is a neurokinin-1 (NK1) receptor antagonist, exhibiting an IC50 of 330 nM. This compound has demonstrated significant biological activity, making it valuable in the research of neurokinin signaling pathways and their roles in various physiological and pathological processes. Vapreotide acetate is commonly utilized in studies involving pain management, cancer therapy, and gastrointestinal disorders. -
Neurokinin Receptor Agonist
Neurokinin B is a neurokinin receptor agonist that belongs to the tachykinin family of peptides. It selectively interacts with G protein-coupled receptors, including neurokinin receptor 1 (NK1R), NK2R, and NK3R, to elicit various physiological responses. This compound has been studied for its roles in pain modulation, neurogenic inflammation, and the regulation of reproductive functions, making it a valuable tool for research in neurobiology and pharmacology. -
Neurokinin Receptor Agonist
Hemokinin 1, human is a selective full agonist of the neurokinin 1 (NK1) receptor, demonstrating significant activity at both NK2 and NK3 receptors as well. This reagent is known for its capacity to induce opioid-independent analgesia, making it a valuable tool in pain research. Hemokinin 1, human can be utilized in studies exploring neurokinin signaling pathways and their implications in various physiological and pathological processes. -
NK-2 Antagonist
MEN 10207 is a selective antagonist of the NK-2 tachykinin receptor, demonstrating significant activity with pA2 values of 5.2, 7.9, and 4.9 across in vitro assays for NK-1, NK-2, and NK-3 receptors, respectively. This compound is primarily utilized in research to elucidate the physiological roles of tachykinins and their associated receptors. MEN 10207 can be instrumental in studies focused on neurogenic inflammation, pain modulation, and various neuropsychiatric disorders. -
NK1 Antagonist
Fosnetupitant chloride monohydrochloride is an NK1 receptor antagonist designed to inhibit neurokinin-1 signaling. It demonstrates high affinity for the human NK1 receptor with a pKi value of 9.5 and exhibits moderate activity at the NK3 receptor with a pKi value of 6.1. This compound serves as a methylene phosphate prodrug of Netupitant, making it a valuable tool for research in the fields of oncology and pain management, particularly for evaluating antiemetic properties and exploring neurokinin-related pathways.
