Catalog No.
Product Name
Application
Product Information
Citations
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Neurokinin Receptor Agonist
[Nle11]-Substance P is an agonist of neurokinin receptors, designed to circumvent the oxidation issues associated with methionine in natural Substance P. This analog exhibits enhanced stability and retains biological activity, making it suitable for research studies focused on pain modulation, neurogenic inflammation, and neuropsychiatric disorders. Its application in various in vitro and in vivo models supports investigations into neurokinin signaling pathways and their implications in therapeutic interventions. -
Reversed Substance P
MLGFFQQPKPR-NH2 is a reversed Substance P peptide that acts as an antagonist to its neuropeptide target. This compound has demonstrated the ability to interfere with neurogenic inflammation and modulate pain response, making it a valuable tool for studies of nociception and neuropeptide signaling. Research applications include investigations into pain mechanisms and the development of potential therapeutic strategies for pain management. -
NK1/NK2 Antagonist
WIN 66306 is a cyclic heptapeptide that acts as an antagonist for neurokinin 1 (NK1) and neurokinin 2 (NK2) receptors. This compound exhibits significant antagonistic activity, making it a valuable tool for studies related to pain, inflammation, and various neurological disorders. Its role in modulating neurokinin signaling pathways supports research applications in pharmacology and neuroscience. -
hNK1 Antagonist
L 743310 is a selective non-peptide antagonist of the human neurokinin 1 (hNK1) receptor, exhibiting high affinity for both primate and cloned human receptors while displaying lower affinity for rodent NK1 receptors. This compound has demonstrated efficacy in inhibiting resiniferatoxin-induced plasma protein extravasation in guinea pig esophagus. Additionally, L 743310 exhibits a dose-dependent inhibitory effect on cisplatin-induced emesis, making it a valuable tool for research in neurokinin signaling and anti-emetic drug development. -
Neurokinin B Analogue
Tyr0-Neurokinin B is a Neurokinin B analogue that primarily targets neurokinin receptors. This compound has been shown to induce contractions in bladder smooth muscle, making it valuable for studying bladder physiology and potential therapeutic applications in urinary disorders. Researchers may utilize Tyr0-Neurokinin B to investigate the role of neurokinins in various biological processes and conditions related to smooth muscle function. -
Neurokinin Receptor Agonist
Scyliorhinin II is a selective neurokinin-3 receptor agonist, exhibiting a Ki value of 2.5 nM for the neurokinin-3 receptor in rat cerebral cortex. This compound plays a significant role in modulating neurogenic inflammatory processes and has potential applications in the study of neurokinin signaling pathways. It is valuable for researching the physiological and pharmacological roles of neurokinin receptors in various biological systems. -
Tachykinin NK1 Receptor Antagonist
GR 82334 is a potent and selective reversible antagonist of the tachykinin NK1 receptor. This compound effectively inhibits substance P-induced sensitization by blocking NK1 receptors, demonstrating its utility in research related to pain modulation and neurobiology. The specific mechanism of action makes GR 82334 a valuable tool for investigating the role of tachykinins in various biological processes and for exploring potential therapeutic applications. -
Neurokinin-1 Receptor Antagonist
SLV-317 is a selective antagonist of the neurokinin-1 receptor, exhibiting oral bioavailability. It effectively inhibits substance P-induced responses, making it a valuable compound for studying neurokinin signaling pathways. This compound is particularly relevant in research focused on pain, anxiety, and other neurogenic conditions. -
NK1/NK3 Antagonist
RO4583298 is a potent dual antagonist of NK1 and NK3 receptors, exhibiting oral bioavailability. This compound effectively inhibits senktide-induced enhancement of the spontaneous activity of dopaminergic neurons, making it valuable for research in neuropharmacology. Additionally, RO4583298 has been shown to block foot tapping responses in gerbils and inhibit tail whips in mice, supporting its utility in behavioral studies related to neurokinin receptor modulation. -
Tachykinin Antagonist
[D-Pro4,D-Trp7,9,10] Substance P (4-11) is a potent antagonist of tachykinin receptors. This peptide plays a crucial role in the modulation of neuropeptide signaling pathways and is utilized in research investigating pain perception, inflammation, and neurogenic processes. Its ability to inhibit tachykinin-mediated activities makes it valuable for studies exploring the therapeutic potential in various neurological disorders. -
Neurokinin Receptor Antagonist
MEN 10208 is a neurokinin A antagonist that effectively targets neurokinin receptors, inhibiting their activity. This compound is primarily utilized in research focused on neurobiology and the regulation of pain, anxiety, and other neurological disorders. MEN 10208 can serve as a valuable tool for exploring the physiological roles of neurokinin signaling in various biological contexts. -
Substance P Antagonist
[D-Pro4,D-Trp7,9] Substance P (4-11) is a potent antagonist of Substance P, targeting neurokinin receptors involved in pain and inflammatory responses. It has been shown to effectively decrease plasma aldosterone concentrations, indicating a role in modulating vascular and endocrine functions. This compound is valuable for research applications focused on pain management, neurobiology, and hormonal regulation. -
NK2 Antagonist
UK-224671 is a selective antagonist of the neurokinin-2 (NK2) receptor. This compound exhibits significant potential in modulating NK2 receptor-related pathways, making it valuable for research focused on neurokinin signaling and its implications in various physiological and pathological conditions. It is noteworthy that UK-224671 is influenced by P-glycoprotein efflux and has limited intrinsic membrane permeability, which may affect its oral bioavailability in experimental contexts. -
NK1 Receptor Antagonist
CP 122721 is an orally active antagonist of the neurokinin-1 (NK1) receptor. It exhibits significant antiemetic effects, effectively reducing cisplatin-induced vomiting in ferrets, with an ID50 of 0.08 mg/kg. Additionally, CP 122721 inhibits kainate-induced seizure activity and protects against CA1 neuronal cell death in rat models. This compound is valuable for research applications in depression, asthma, and irritable bowel syndrome (IBS). -
NK-1 Receptor Antagonist
L-733060 is a selective neurokinin-1 (NK-1) receptor antagonist that effectively inhibits the binding of Substance P to its receptor. This compound modulates pain transmission and neural plasticity, making it particularly relevant for chronic pain research. L-733060 has demonstrated efficacy in reversing orofacial hyperalgesia and inhibits neurogenic plasma extravasation without causing cardiovascular side effects in animal models. Its potential applications extend to studies involving chronic orofacial pain and neurogenic inflammation. -
Neurokinin 2 Receptor Agonist
L 363851 is a potent agonist of the neurokinin 2 receptor, demonstrating a significant contractile response in tracheal smooth muscle tissue devoid of epithelium with an IC50 value of 3.2 nM. Additionally, it stimulates phosphoinositide hydrolysis with an IC50 of 36 μM. This compound is valuable for research applications focusing on respiratory physiology and neurogenic inflammation. -
Substance P Agonist
Substance P (4-11) is a Substance P agonist that specifically targets and activates NK1 receptors. This C-terminal fragment of Substance P exhibits potent biological activity, making it valuable for research in neurobiology, pain modulation, and inflammation. Its selective interaction with NK1 receptors offers insights into neurokinin signaling pathways and potential therapeutic applications. -
NK-1 Receptor Antagonist
Lanepitant is a selective neurokinin-1 (NK-1) receptor antagonist. It inhibits neurogenic inflammation and pain transmission by blocking the interaction of substance P with NK-1 receptors found in both neuronal and non-neuronal tissues. Lanepitant is particularly useful in research related to osteoarthritis and understanding pain mechanisms. -
Substance P Inhibitor
[D-Pro2,D-Phe7,D-Trp9] Substance P is a synthetic analogue of Substance P that functions as a potent inhibitor of the neuropeptide. It exhibits a significant ability to modulate neurogenic inflammation and pain response by blocking Substance P-mediated signaling pathways. This compound is useful in studying the role of Substance P in pain and gastrointestinal motility research applications, particularly in models involving guinea-pig ileum contraction. -
Neurokinin Receptor Agonist
C14TKL-1 is a tachykinin-like peptide that acts as an agonist for neurokinin receptor 1 (NK-1). This compound is utilized in research to study the physiological roles of NK-1 in neurogenic inflammation and pain pathways. Its activity may provide insights into the underlying mechanisms of various neurological disorders and potential therapeutic targets. -
Histamine Methylated Product
3-Methylhistamine dihydrochloride is a methylated derivative of histamine that serves as a significant biomarker in the study of immune responses. This compound has been shown to be upregulated in vaccinated murine models, making it useful for research applications focused on immunological studies and histamine-related pathways. Its role in the modulation of immune activity positions it as a valuable reagent in exploring allergic reactions and other histamine-mediated processes. -
Endogenous Metabolite
8-(3-Chlorostyryl)caffeine is a selective antagonist of the A2a adenosine receptor, demonstrating a significant 520-fold selectivity in radioligand binding assays conducted in rat brain. It effectively inhibits adenylylase with a 22-fold selectivity in rat chromaffin cells. Co-administration with the A1-selective antagonist CPX has been shown to enhance exercise activity. Additionally, 8-(3-Chlorostyryl)caffeine exhibits potent inhibitory activity against MAO-B in primate mitochondrial systems. This compound serves as a valuable tool for studying adenosine receptor signaling and its effects on physiological processes. -
Endogenous Metabolite
Palmitoleoyl ethanolamide (POEA) is an endogenous fatty amide that functions primarily as a signaling molecule through the activation of cannabinoid receptors. It has been shown to exhibit anti-inflammatory and analgesic properties, making it relevant for research in pain management and inflammatory disorders. POEA's involvement in metabolic processes also positions it as a valuable target for studies in obesity and metabolic syndrome. -
Endogenous Metabolite
5-OAHSA is an endogenous metabolite that functions as a lipid mediator. It is known to lower blood glucose levels, enhance glucose tolerance, and stimulate the secretion of glucagon-like peptide-1 (GLP-1) and insulin. 5-OAHSA is valuable for research applications focused on metabolic regulation and inflammation modulation. -
Endogenous Metabolite
Hydroxy bosentan is an endogenous metabolite derived from Bosentan, primarily processed by the cytochrome P450 system in the liver. This compound retains 10%-20% of Bosentan's pharmacological activity, serving as a significant contributor to the overall therapeutic effects of the parent compound. Hydroxy bosentan is useful in research focused on metabolic pathways and the pharmacokinetics of endothelin receptor antagonists. -
Endogenous Metabolite
1-Methylhistamine dihydrochloride is a metabolite of histamine that primarily targets histamine receptors. This compound exhibits significant biological activity in the modulation of allergic responses and neurotransmission processes. It is widely utilized in research applications focusing on histamine signaling pathways and its role in various physiological and pathological conditions. -
Drug Metabolite
Desmethyl Bosentan is an active metabolite of the endothelin receptor antagonist bosentan. It functions primarily by activating the pregnane X receptor (PXR), as demonstrated in CV-1 monkey kidney cells expressing the human receptor in a reporter assay at a concentration of 25 μM. This compound is valuable for studying drug metabolism and the regulatory pathways involved in pharmacokinetics and toxicology research. -
DAGL-α/DAGL-β Inhibitor
LEI105 is a selective and reversible dual inhibitor of diacylglycerol lipase (DAGL)-α and DAGL-β. This compound effectively decreases levels of 2-arachidonoylglycerol in Neuro2A cells, demonstrating its potential to modulate endocannabinoid signaling. Research applications include investigations into the mechanisms underlying obesity, metabolic disorders, and neuroinflammation, as well as studies of cannabinoid receptor-mediated synaptic plasticity in mouse hippocampal slices. -
Drug Metabolite
Quetiapine sulfoxide dihydrochloride is a primary metabolite of the second-generation antipsychotic quetiapine. This compound functions as a 5-HT receptor agonist and a dopamine receptor antagonist, contributing to its pharmacological effects. It is commonly utilized in research related to neuropharmacology and metabolic profiling of antipsychotic drugs, offering insights into the drug's therapeutic activity and safety profile. -
Metabolite of Acebutolol
Diacetolol is an active metabolite of the beta-adrenoceptor antagonist Acebutolol. It exhibits pharmacological activity by selectively inhibiting β1-adrenergic receptors, which plays a significant role in cardiovascular research. Diacetolol is utilized to study beta-blocker pharmacodynamics and to explore its effects on heart rate and blood pressure regulation. -
Drug Metabolite
3-Hydroxy Medetomidine is a primary metabolite of the α2-adrenergic receptor agonist medetomidine. This compound exhibits important biological activity as it participates in modulating adrenergic signaling pathways. Research applications include studies on drug metabolism and the pharmacokinetics of sedatives in both veterinary and medical contexts. -
Lurasidone Metabolite
Lurasidone Metabolite 14283 hydrochloride is a significant active metabolite of the antipsychotic agent Lurasidone, which targets serotonin and dopamine receptors. This compound plays a crucial role in the pharmacological activity of Lurasidone, contributing to its efficacy in the treatment of schizophrenia. Research applications include studying the metabolic profile of Lurasidone and its pharmacodynamics in neural systems. -
5-HT2A Inverse Agonist
N-Desmethyl Pimavanserin is a potent inverse agonist of the 5-HT2A receptor, serving as an active metabolite of Pimavanserin. With high affinity demonstrated by a pIC50 of 8.73 and pKd of 9.3, this compound has significant implications in research focused on psychiatric disorders, such as schizophrenia and Parkinson's disease psychosis. Its role in modulating serotonergic signaling makes it an important reagent for studies investigating the therapeutic potential of 5-HT2A antagonism. -
Drug Metabolite
Quetiapine sulfoxide hydrochloride is a primary metabolite of Quetiapine, a second-generation antipsychotic. This compound acts primarily as a 5-HT receptor agonist and dopamine receptor antagonist, contributing to the pharmacological profile of Quetiapine. It is valuable in research focusing on the metabolism and pharmacokinetics of antipsychotic medications, providing insights into their therapeutic effects and potential side effects. -
Drug Metabolite
1-epi-Regadenoson is an α-isomer impurity of Regadenoson, a potent and selective agonist for the adenosine A2A receptor. This compound is primarily used in research to investigate the pharmacological effects of adenosine receptor activation and its implications in cardiovascular function. The study of 1-epi-Regadenoson can aid in understanding the metabolic pathways and potential therapeutic effects associated with adenosine receptor modulation. -
Active Metabolite of delta 9-Tetrahydrocannabinol
9α,10α-Epoxyhexahydrocannabinol is an active metabolite of delta 9-tetrahydrocannabinol, primarily targeting cannabinoid receptors. This compound exhibits notable anticonvulsant properties, effectively reducing body temperature and prolonging pentobarbital-induced sleep in animal models. Additionally, it has demonstrated protective effects against pentylenetetrazol-induced seizures, making it valuable for research in seizure disorders and cannabinoid pharmacology. -
H1-Receptor Antagonist
Cetirizine Impurity B dihydrochloride is an impurity of the H1-receptor antagonist, cetirizine dihydrochloride. While cetirizine demonstrates significant antiallergic properties and effectively inhibits eosinophil chemotaxis during allergic responses, this specific impurity is valuable for analytical purposes and quality control in research applications. It aids researchers in understanding the pharmacological profile and potential effects associated with cetirizine and its metabolites. -
Quetiapine Metabolite
7-Hydroxyquetiapine is the primary active metabolite of the antipsychotic agent Quetiapine. It functions by modulating various neurotransmitter systems, particularly serotonin and dopamine receptors, contributing to its therapeutic effects in managing psychiatric disorders. This compound is valuable for studying the pharmacological profile of Quetiapine and investigating its metabolic pathways in both in vitro and in vivo research settings. -
Drug Metabolite
Silodosin Glucuronide sodium is the sodium salt of Silodosin β-D-glucuronide, a metabolite of the selective α1A-adrenergic receptor antagonist Silodosin. It exhibits high affinity for the α1A-AR, facilitating a Ki value of 0.036 nM. This compound is crucial for studying the pharmacokinetics and metabolic pathways of Silodosin, contributing to research applications in urology and cardiovascular studies. -
Terbutaline Derivative
Terbutalone is a derivative of terbutaline, targeting the β2-adrenergic receptors. As an orally active agonist, it demonstrates significant bronchodilator activity, making it a valuable tool in asthma and respiratory research. Terbutalone may also have applications in studying other β2-adrenergic receptor-mediated physiological responses. -
Drug Metabolite
Carvedilol Glucuronide is a significant metabolite of the β/α-1 adrenergic receptor antagonist, Carvedilol. This compound demonstrates key biological activity by modulating β-adrenergic signaling and exhibits potential application in studying the metabolic pathway of Carvedilol. Research indicates that Carvedilol can inhibit lipid peroxidation and has properties as an antihypertensive agent, as well as an autophagy inducer that affects the NLRP3 inflammasome. Carvedilol Glucuronide serves as an important reagent for investigating drug metabolism and pharmacokinetics in cardiovascular research. -
Endogenous Metabolite
AZD-3199 is an ultra-long-acting beta2 adrenergic agonist primarily targeting the beta2 adrenergic receptor. It exhibits significant bronchodilator activity, making it a candidate for therapeutic use in asthma and chronic obstructive pulmonary disease (COPD) research. Its prolonged action facilitates investigations into novel treatment strategies for managing these respiratory conditions. -
Drug Derivative
Bmapn is a drug derivative with impactful interactions on dopamine signaling pathways. It exhibits rewarding and reinforcing properties by decreasing dopamine transporter levels and enhancing dopamine receptor D2 gene expression specifically in the striatum. This compound is valuable for research applications studying addiction, neuropharmacology, and the modulation of dopaminergic systems. -
Stable Isotope
Boc-Leu-OH·H2O-13C is a stable isotope-labeled derivative of N-Boc-L-leucine, featuring a carbon-13 (13C) label. This amino acid derivative, protected with a Boc group, serves as an essential building block for the synthesis of peptides, such as L-prolyl-L-leucyl-glycinamide, which exhibit modulatory activity on dopamine receptors. It is valuable for applications in peptide research, metabolic studies, and tracer experiments utilizing stable isotopes. -
Histamine N-methyltransferase
Histamine N-methyltransferase, rat is a biocatalyst that functions primarily by catalyzing the N-methylation of histamine. This enzyme plays a critical role in the metabolism of histamine, contributing to the regulation of physiological processes such as inflammatory responses and neurochemical signaling. Research applications include enzyme engineering aimed at optimizing reaction kinetics, enhancing substrate specificity, and improving enzyme stability under varying pH conditions, potentially facilitating dynamic control of enzymatic activity for various experimental needs. -
Activation Peptide
Enterostatin (rat) is an activation peptide of procolipase that plays a significant role in modulating fat intake. This peptide selectively reduces body fat consumption and lowers serum cholesterol levels through a cholecystokinin 1 (CCK1) receptor-dependent mechanism. It serves as a valuable tool for research on energy balance, appetite regulation, and metabolic disorders. -
N-acylserinol Compound
Myristoyl ethanolamide, an N-acylserinol compound, functions as a bioactive lipid signaling molecule. It is involved in modulating various biological processes, including inflammation and pain perception. Myristoyl ethanolamide serves as a valuable tool in research applications focused on lipid metabolism, neuromodulation, and the study of cannabinoid receptor interactions. This compound can enhance the understanding of endocannabinoid signaling pathways and their implications in physiological and pathological conditions. -
Blood Platelet Aggregation Inhibitor
Ent-8-Iso-15(S)-prostaglandin F2α is a potent inhibitor of blood platelet aggregation. This compound exhibits superior activity compared to its isomer, 8-Isoprostaglandin F2α, in whole blood assays, making it a valuable tool for studying platelet function and related cardiovascular research. Its mechanism of action can aid in the exploration of therapeutic strategies for conditions associated with abnormal platelet aggregation. -
PROTAC Linker
2-[4-(Aminomethyl)triazol-1-yl]ethanamine is a specialized PROTAC linker that serves as a crucial component in targeted protein degradation strategies. This compound facilitates the synthesis of PROTAC CB1R Degrader-1, enabling the effective modulation of cannabinoid receptor 1 (CB1R) levels. Its application in research supports investigations into protein homeostasis and therapeutic approaches for various diseases. -
Ligand for Target Protein for PROTAC
Rimonabant carboxylic acid is a ligand used for the targeted protein degradation (PROTAC) approach by engaging with the target protein. This compound plays a crucial role in synthesizing PROTAC CB1R Degrader-1, facilitating the study of cannabinoid receptor biology and influencing metabolic processes. It serves as a valuable tool for researchers investigating innovative therapeutic strategies for conditions related to the endocannabinoid system.
