Catalog No.
Product Name
Application
Product Information
Citations
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Opioid Compound
Bipiperidinyl 4-ANPP is an opioid compound that interacts primarily with the mu-opioid receptor. This compound demonstrates significant analgesic properties and is utilized in research focused on pain management and opioid receptor pharmacology. Its structural similarity to known opioids positions it as a valuable tool for investigating the mechanisms underlying opioid action and potential therapeutic applications in chronic pain and addiction studies. -
μ-Opioid Receptor Agonist
Endomorphin 2 is a high-affinity agonist of the μ-opioid receptor, exhibiting selectivity and potency in targeting this pathway. It also shows moderate affinity for kappa3 binding sites, with a Ki value ranging from 20 to 30 nM. This compound is valuable for research in pain management, neurobiology, and the pharmacological characterization of opioid receptors. Its unique properties make it suitable for studies focused on opioid signaling and potential therapeutic applications in pain relief. -
Orexin Receptor Agonist
Danavorexton is an orexin receptor agonist with notable brain permeability. This compound selectively activates the OX2R receptor, demonstrating efficacy in enhancing wakefulness and alleviating symptoms of sleepiness in preclinical models. Danavorexton serves as a valuable tool for research into sleep disorders and the pharmacological modulation of the orexin system. -
Alixorexton Enantiomer
Alixorexton enantiomer is a selective, orally active agonist targeting the orexin-2 receptor. This compound is primarily investigated for its potential applications in the study of hypersomnias and related sleep disorders. Its ability to penetrate the blood-brain barrier makes it a valuable tool for exploring orexin system functioning and its implications in sleep regulation. -
OX Receptor Antagonist
EMPA is a selective and reversible antagonist of the orexin OX2 receptor. It demonstrates high-affinity binding, with KD values of 1.1 nM for human and 1.4 nM for rat OX2-HEK293 membranes. This compound is valuable for research into the role of orexin signaling in various physiological processes and related disorders. -
Orexin Type 2 Receptor Agonist
Oveporexton is a selective agonist of the orexin type 2 receptor (OX2R) with an EC50 of 2.5 nM and demonstrates a remarkable 3000-fold selectivity over the orexin type 1 receptor (OX1R). This compound is particularly relevant for research into hypersomnia disorders, including narcolepsy, providing insights into sleep regulation and potential therapeutic approaches. Its oral bioactivity enables convenient experimental application in various preclinical studies. -
OX1R/OX2R Antagonist
Vornorexant is a potent antagonist of both the OX1R and OX2R receptors, exhibiting IC50 values of 1.05 nM and 1.27 nM, respectively. This compound is primarily utilized in studies focused on sleep physiology and insomnia, demonstrating significant sleep-promoting effects in vivo. It serves as a valuable tool for researchers investigating the pathophysiology of sleep disorders and the therapeutic potential of orexin receptor modulation. -
OX2R Activator
Alixorexton is a selective OX2R activator that effectively crosses the blood-brain barrier, functioning as a wake-promoting agent. This compound is primarily utilized in research related to sleep disorders, including narcolepsy and idiopathic hypersomnia, making it a valuable tool for investigating the mechanisms of sleep regulation and potential therapeutic interventions. -
Orexin Receptor 2 Agonist
YNT-185 is a selective agonist of the orexin type-2 receptor (OX2R), exhibiting an EC50 of 0.028 μM for OX2R and 2.75 μM for OX1R. This nonpeptide compound has been shown to alleviate symptoms of narcolepsy-cataplexy in murine models, making it a valuable tool for researching sleep disorders and neurodegenerative conditions related to orexin signaling. -
Orexin-2 Receptor Antagonist
Seltorexant hydrochloride is a selective antagonist of the orexin-2 receptor (OX2R), exhibiting high affinity characterized by pKi values of 8.0 and 8.1 in human and rat OX2R, respectively. This compound is capable of permeating the blood-brain barrier and effectively occupies OX2R binding sites in the rat brain. Seltorexant hydrochloride is valuable for research applications focused on sleep disorders and the modulation of wakefulness, making it a pertinent tool in neuroscience studies. -
Orexin Receptor 2 Agonist
YNT-185 dihydrochloride is a selective agonist of the orexin type-2 receptor (OX2R), demonstrating an EC50 of 0.028 μM for OX2R and 2.75 μM for OX1R. This compound has shown efficacy in ameliorating symptoms associated with narcolepsy-cataplexy in murine models, making it a valuable tool for research in sleep disorders and related pathophysiologies. Its selectivity for OX2R positions YNT-185 dihydrochloride as a significant reagent for exploring orexin receptor mechanisms and therapeutic interventions. -
Orexin Receptor Agonist
Orexin B is an endogenous agonist for the orexin receptors, exhibiting a Ki of 420 nM for the OX1 receptor and 36 nM for the OX2 receptor. This peptide plays a crucial role in regulating various physiological processes, including energy homeostasis, sleep-wake cycles, and appetite. Orexin B is primarily utilized in research applications focused on neurobiology and metabolic diseases, providing insights into the mechanisms of sleep regulation and potential therapeutic targets for disorders like narcolepsy and obesity. -
Orexin Receptor Antagonist
ACT-462206 is a potent dual antagonist of the Orexin 1 and Orexin 2 receptors, demonstrating IC50 values of 60 nM and 11 nM, respectively. This orally active compound exhibits favorable brain penetration, making it suitable for research into insomnia, anxiety disorders, and addiction. Its targeted mechanism allows for exploration of orexin signaling pathways and their role in regulating sleep and stress responses. -
Orexin 1 Receptor Agonist
(R)-YNT-3708 is a selective agonist of the orexin 1 receptor (OX1R), exhibiting an EC50 of 7.48 nM. This compound demonstrates significant antinociceptive effects, making it a valuable tool for research in pain modulation and potential therapeutic applications in disorders related to orexin signaling. -
Orexin-1 Receptor Antagonist
CVN766 is an orally active orexin-1 receptor antagonist, exhibiting an IC50 of 8 nM for OX1R and greater than 10 μM for OX2R, indicating selectivity. This compound demonstrates effective blood-brain barrier permeability, making it suitable for neurological studies. CVN766 is primarily utilized in research related to schizophrenia, providing insights into the role of orexin receptors in neuropsychiatric disorders. -
OX1R Antagonist
JNJ-54717793 is a selective and high-affinity antagonist of the orexin-1 receptor (OX1R), demonstrating significant brain penetration and oral bioactivity with a plasma EC50 of 85 ng/mL. Its Ki values for the human OX1R and OX2R are 16 nM and 700 nM, respectively. This compound is primarily utilized in research on anxiety disorders, providing insights into the modulation of orexin signaling pathways. -
OX40 Agonist Antibody
Ordastobart is a hexavalent OX40 agonist antibody that enhances OX40 receptor clustering and signaling. This mechanism leads to increased proliferation and activation of CD4+ and CD8+ T cells both in vitro and in vivo. Ordastobart demonstrates anti-tumor activity and has been shown to improve survival in mouse models of cancers, such as fibrosarcoma and colorectal cancer. It is suitable for research applications focusing on cancer immunotherapy. -
Orexin Receptor Antagonist
Fazamorexant is a dual orexin receptor antagonist targeting both OX1R and OX2R, with IC50 values of 32 nM and 41 nM, respectively. This compound is known to enhance total sleep time and improve sleep efficiency, making it a valuable tool for the study of insomnia and sleep disorders. Fazamorexant is suitable for use in various research applications focused on therapeutic strategies for sleep-related conditions. -
Orexin Type 2 Receptor Agonist
Suntinorexton is an Orexin Type 2 Receptor (OX2R) agonist that modulates neuropeptide signaling. This compound enhances respiratory function during sleep, making it valuable for research on sleep disorders and respiratory physiology. Suntinorexton can be utilized to investigate the role of the orexin system in regulating wakefulness, arousal, and metabolic processes. -
OX2 Agonist
[Ala11,D-Leu15]-Orexin B (human) is a selective agonist of the orexin-2 receptor (OX2), exhibiting a significant 400-fold selectivity for OX2 with an EC50 of 0.13 nM compared to OX1 (52 nM). This compound plays a critical role in the regulation of arousal, sleep, and appetite. It is widely used in research applications aimed at understanding the neurobiology of sleep disorders and metabolic conditions. -
OX1R Inhibitor
Tebideutorexant is a selective inhibitor of the orexin receptor 1 (OX1R), demonstrating significant oral bioavailability and the ability to cross the blood-brain barrier. With a human OX1R pKi of 8.17 and a rat OX1R pKi of 8.13, this compound specifically targets OX1R while exerting minimal effects on OX2R. Tebideutorexant is a valuable tool for investigating panic and anxiety disorders in preclinical research settings. -
Isomer
(2R,3R)-Firazorexton is a selective agonist of the orexin type 2 receptor (OX2R), known for its potential to enhance wakefulness and alleviate symptoms associated with narcolepsy. As an isomer of Firazorexton, this compound exhibits the same brain-penetrating properties, making it suitable for research in sleep disorders and circadian rhythm regulation. Its biological activity supports investigations into therapeutic avenues for energy balance and long-term wakefulness. -
Orexin 2 Agonist
Orexin 2 Receptor Agonist 2 is a selective agonist of the orexin 2 receptor, facilitating the activation of this neuropeptide receptor involved in regulating arousal, appetite, and wakefulness. This compound is valuable for research applications related to sleep disorders, obesity, and neurodegenerative diseases. Its specificity for the orexin 2 receptor makes it a crucial tool for exploring the physiological and pharmacological roles of orexin signaling pathways. -
Orexin Receptor (OX Receptor) Antagonist
Orexin receptor antagonist 2 is a selective antagonist of the orexin receptors (OX receptors), exhibiting potent inhibitory activity with pKis of 7.69 and 9.78. This compound is valuable for research into sleep disorders, particularly insomnia, by providing insights into the modulation of orexin signaling pathways involved in the regulation of arousal and wakefulness. -
YNT-3708 S-enantiomer
(S)-YNT-3708 is the S-enantiomer of YNT-3708, exhibiting low affinity for both the orexin receptor type 1 (OX1R) and orexin receptor type 2 (OX2R), with EC50 values of 3595 nM and 1661 nM, respectively. Its low receptor activity makes it a useful tool for studies investigating orexin pathway modulation and its implications in sleep regulation and energy homeostasis. This compound can be applied in pharmacological research aimed at understanding the role of orexin receptors in various biological processes. -
OX40 Activator
Efizonerimod alfa is a potent monoclonal antibody that functions as an OX40 activator. This reagent enhances T-cell activation and proliferation, making it particularly relevant for cancer research and immunotherapy studies. Its ability to modulate immune responses positions it as a valuable tool for investigating therapeutic strategies in oncology. -
Orexin Receptor (OX Receptor) Antagonist
Orexin receptor antagonist 3 functions as an antagonist of the orexin receptors, specifically targeting OX receptors. This compound can modulate the activity of orexin, playing a significant role in the regulation of sleep-wake cycles and appetite. It is employed in research applications focused on sleep disorders, metabolic syndromes, and other conditions influenced by orexin signaling. -
Dual Orexinergic Receptor Antagonist
DORA-22 is a dual orexinergic receptor antagonist that targets orexin receptors OX1 and OX2, playing a critical role in regulating arousal, sleep, and appetite. It effectively alleviates sleep disruption and addresses memory impairment associated with sleep disorders. DORA-22 is useful for research applications related to insomnia and other sleep-related conditions. -
Appetite Suppressant
GYKI-13380 is an appetite suppressant that acts primarily on neurochemical pathways involved in energy balance and hunger regulation. This compound demonstrates potential for study in neurological disorders related to appetite and metabolism. Researchers can utilize GYKI-13380 to explore its effects on weight management and the underlying mechanisms of appetite control. -
OX2R Agonist
OX-201 is a potent OX2R agonist that effectively crosses the blood-brain barrier, exhibiting an EC50 of 8.0 nM. This compound stimulates OX2R, leading to increased wakefulness and neuronal activation. Additionally, OX-201 facilitates the release of activity-dependent tau protein from neurons into the interstitial fluid of hippocampal tissues. It is a valuable tool for research into Alzheimer's disease and tauopathies. -
OX2R Antagonist
OX2-2303 is a potent and selective antagonist of the orexin-2 receptor (OX2R), demonstrating exceptional binding affinity with a Ki value of 0.1 nM and over 890-fold selectivity for OX2R compared to OX1R. This compound is valuable for applications in central nervous system (CNS) research, particularly as a positron emission tomography (PET) radioligand, enabling the study of OX2R's role in various neurological processes. -
OX2R Agonist
Cleminorexton is an orally active agonist of the orexin-2 receptor (OX2R), exhibiting a pEC50 value between 9 and 10.4. This compound is primarily utilized in research related to narcolepsy and other disorders characterized by orexin deficiency and excessive daytime sleepiness. Its modulation of OX2R activity makes it a valuable tool for studying sleep-wake regulation and potential therapeutic interventions. -
Orexin Receptor Modulator
Orexin receptor modulator-1 is a selective modulator of orexin receptors, playing a vital role in the regulation of arousal, wakefulness, and appetite. It demonstrates significant biological activity in the context of substance addiction, anxiety, depression, and various stress-related disorders. This compound serves as a valuable tool for investigating the pathophysiology of disorders such as post-traumatic stress disorder, panic disorder, and seasonal affective disorder, as well as the modulation of pain and hypertension. -
OX2R Agonist
Ledasorexton is a potent oral agonist of the OX2 receptor (OX2R), exhibiting an EC50 of 0.99 nM. This compound has been demonstrated to induce wakefulness and promote alertness, making it a valuable tool for research into sleep regulation and associated disorders. Its specificity for the OX2R highlights its potential applications in studying neurobiology and pharmacology related to sleep and wakefulness. -
Orexin Receptor Agonist
Orexin receptor activator-1 is an agonist for the orexin receptor. This compound exhibits biological activity by modulating orexin signaling pathways, making it valuable for studying orexin-related disorders such as narcolepsy and obesity. Its application extends to research on sleep regulation and energy homeostasis, contributing to the understanding of various neurophysiological processes. -
OX2R Agonist
OX2R-IN-3 is a potent agonist of the type 2 orexin receptor (OX2R) with an EC50 value of less than 100 nM. This compound demonstrates significant biological activity in modulating orexin signaling pathways, making it a valuable tool for research in sleep disorders, energy homeostasis, and neurodegenerative diseases. OX2R-IN-3 can facilitate the exploration of OX2R-related functions in various physiological and pathological contexts. -
OXR Agonist
YNT-3708 is an orexin receptor (OXR) agonist that demonstrates selective activation of OX1R and OX2R. It has EC50 values of 14.6 nM for OX1R and 277 nM for OX2R, making it a valuable tool for studying orexin signaling pathways. This compound is primarily utilized in research applications related to sleep regulation, appetite control, and neurodegenerative diseases. -
OX2R Antagonist
Fumiporexant is a selective antagonist of the Orexin receptor 2 (OX2R), demonstrating oral bioavailability and effective penetration into the brain. This compound modulates the sleep-wake cycle and influences emotion-related pathways within the central nervous system. Fumiporexant is of significant interest in the study of neurological disorders, particularly insomnia and major depressive disorder. -
Orexin Receptor Activator
Xenopus orexin A acts as a potent agonist of the orexin receptor OX1R, functioning as a neuropeptide that binds to G-protein-coupled receptors. This endogenous ligand plays a critical role in modulating various physiological processes, including appetite regulation and arousal. Research applications of Xenopus orexin A include studying energy homeostasis, sleep-wake cycles, and potential implications in metabolic disorders. -
OX2R Antagonist
Orexin receptor antagonist 4 is a potent and selective antagonist of the orexin 2 receptor (OX2R), exhibiting an IC50 of 4.27 nM. This compound demonstrates a notable 61-fold selectivity for OX2R over the orexin 1 receptor (OX1R), which has an IC50 of 295 nM. Orexin receptor antagonist 4 is valuable for research applications exploring the role of orexin signaling in sleep regulation, energy metabolism, and various neurobiological processes. -
Orexin Receptor Agonist
Xenopus orexin B is a neuropeptide that acts as an agonist for the orexin receptor, specifically OX2R. This compound plays a crucial role in regulating various physiological processes, including arousal, appetite, and energy homeostasis. Its ability to activate orexin receptors makes it a valuable tool for research investigating sleep-wake cycles, metabolic disorders, and neurodegenerative diseases. -
Orexin Receptor (OX Receptor) Agonist
Orexin B (human) is an endogenous agonist that selectively targets the Orexin receptors, OX1 and OX2, with inhibition constants (Kis) of 420 nM and 36 nM, respectively. This compound plays a critical role in regulating arousal, appetite, and energy homeostasis. Orexin B is widely used in research applications focused on sleep disorders, metabolic syndromes, and neurodegenerative diseases, making it an essential tool for understanding Orexin signaling pathways. -
OX2R Antagonist
OX2R-IN-1 is a selective antagonist of the OX2 receptor (OX2R), exhibiting a low cytotoxicity profile. With an IC50 value of 484 μM, it serves as a potential binder for OX2R studies. Notably, OX2R-IN-1 demonstrates the ability to penetrate the blood-brain barrier (BBB) and possesses a short half-life, making it suitable for research applications targeting central nervous system functions and disorders. -
RNAi
DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite is an RNAi agent that specifically targets and inhibits Ataxin-2 (ATXN2). This compound plays a critical role in research focused on ATXN2-associated neurological disorders, facilitating the study of gene silencing mechanisms and potential therapeutic interventions. Its application may enhance understanding of disease pathways related to ATXN2. -
OX1R Antagonist
Orexin receptor antagonist 7 selectively targets the orexin receptor 1 (OX1R) with a Ki value of 4.05 nM, demonstrating potent antagonistic activity. This compound shows negligible affinity for the orexin receptor 2 (OX2R) and minimal binding to opioid receptors (μ, δ, κ) with Ki values exceeding 1,000 nM. Orexin receptor antagonist 7 is suitable for research applications focused on opioid addiction and the elucidation of orexin-related pathways in various physiological and pathological contexts. -
OX1 Receptor Antagonist
Rocavorexant is a selective antagonist of the orexin-1 receptor (OX1) with a pIC50 of 9.1 for human OX1 and a pIC50 of 6.0 for human OX2. This compound effectively inhibits the signaling pathways associated with orexin receptors, making it a valuable tool for investigating sleep disorders, appetite regulation, and related neurological conditions. Rocavorexant is utilized in research studies aimed at understanding the physiological roles of orexin signaling and for the development of therapeutic strategies targeting these pathways. -
OX2R Agonist
OX2R Agonist 1 is a selective agonist of the orexin receptor 2 (OX2R), exhibiting an effective concentration (EC50) of less than 100 nM. This compound is instrumental in studying the neurobiology of sleep regulation and is particularly relevant for research focused on excessive daytime sleepiness and narcolepsy. Its potent biological activity positions it as a valuable tool in the exploration of treatments for sleep disorders. -
OX1 Antagonist
Orexin receptor antagonist 6 selectively targets the orexin 1 receptor (OX1) with a potent Ki of 8.5 nM and demonstrates more than 1180-fold selectivity for the OX2 receptor. This compound does not elicit conditioned place preference (CPP) or aversive effects and effectively inhibits CPP induced by psychoactive substances. Orexin receptor antagonist 6 is a valuable tool for investigating the role of orexin signaling in neurological diseases and related research applications. -
Orexin 1/2 Receptor Antagonist
DORA 42 is a dual antagonist of the orexin 1 and orexin 2 receptors. It demonstrates significant efficacy in promoting sleep in rat models, highlighting its potential utility in insomnia research. This compound serves as an important tool for studying the role of orexin receptors in sleep regulation and related disorders.
