Catalog No.
Product Name
Application
Product Information
Citations
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OX Antagonist
Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. -
orexin receptor antagonist
Nemorexant (ACT-541468) is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively. -
OX1 receptor antagonist
SB 334867 is a selective non-peptide orexin OX1 receptor antagonist. pKb values are 7.2 and < 5 for inhibition of intracellular Ca2+ release in CHO cells expressing human OX1 and OX2 receptors respectively. Blocks orexin-A induced grooming and feeding following systemic administration in vivo.- Ines M Amaral, .et al. , Psychopharmacology (Berl), 2024, Sep 20 PMID: 39302438
- Tony Ngo, .et al. , Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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Orexin receptor antagonist
MK6096, also known as filorexant, is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R currently in clinical development for insomnia. MK-6096 demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (<3 nM in binding, 11 nM in FLIPR), with no significant off-target activities against a panel of >170 receptors and enzymes.- Mahtab Moshirpour, .et al. , Neuroscience, 2025, May 14:574:114-123 PMID: 40194656
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Dual orexin receptor antagonist
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).- Tung-Yen Lee, .et al. , Front Psychiatry, 2023, Jun 29;14:1196994 PMID: 37457782
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OX2 receptor antagonist
JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 μM for OX1R). -
OX1/OX2 Antagonist
Almorexant HCl is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor 3.- Ryan J Keenan, .et al. , Br J Pharmacol, 2022, Jul;179(13):3403-3417 PMID: 35112344
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OX Receptor Antagonist
SB408124 Hcl is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor. -
Orexin 2 receptor agonist
A potent and selective Orexin2 receptor agonist. -
orexin OX1 receptor antagonist
SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. -
OX2 receptor antagonist
TCS-OX2-29 is a selective OX2 receptor antagonist with IC50 value of 40 nM. CAS: 1610882-30-8 (HCl) 372523-75-6 (Free Base) -
OX2R antagonist
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). -
OX2R antagonist
TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1. -
OX2R agonist
Firazorexton (TAK-994 free base) is an orally active, brain-penetrant, and highly selective agonist of the orexin type 2 receptor (OX2R). By activating OX2R, Firazorexton enhances wakefulness and has demonstrated efficacy in preclinical models, notably improving narcolepsy-like symptoms in mice. Its targeted action on the orexin system positions it as a promising therapeutic candidate for sleep disorders such as narcolepsy and excessive daytime sleepiness. -
OX2R agonist
Firazorexton hydrate (TAK-994) is an orally active, brain-penetrant selective agonist of the orexin type 2 receptor (OX2R). It effectively promotes wakefulness by stimulating OX2R signaling, which plays a critical role in regulating the sleep–wake cycle. In preclinical studies, Firazorexton hydrate has demonstrated the ability to alleviate narcolepsy-like symptoms in mouse models, making it a promising therapeutic candidate for sleep disorders such as narcolepsy and excessive daytime sleepiness. -
Orexin Receptor Agonist
RTIOXA-43 is an orexin receptor agonist that exhibits potent activity with EC50 values of 24 nM for both OX1 and OX2 receptors. This compound is valuable for research applications related to sleep regulation, appetite control, and energy metabolism. By activating orexin receptors, RTIOXA-43 facilitates investigations into neurodegenerative diseases and sleep disorders. -
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.
