Orexin Receptors

Cat. No.

A62717

CAS No.

1628843-99-1

JNJ-54717793

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.

Cat. No.

A62719

CAS No.

1808918-69-5

Fazamorexant

Synonyms: YZJ-1139

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.

Cat. No.

A62725

CAS No.

1457940-75-8

Orexin receptor antagonist 2

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.

Cat. No.

A62728

CAS No.

1293282-55-9

Orexin receptor antagonist 3

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.

Cat. No.

A62729

CAS No.

1088991-95-0

DORA-22

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.

Cat. No.

A62732

CAS No.

1607428-33-0

OX2-2303

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.

Cat. No.

A62739

CAS No.

2839408-03-4

Fumiporexant

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.

Cat. No.

A62741

CAS No.

2251017-69-1

Orexin receptor antagonist 4

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.

Cat. No.

A62745

CAS No.

2639148-08-4

OX2R-IN-1

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.

Cat. No.

A62748

CAS No.

2115665-09-1

Rocavorexant

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.

Cat. No.

A62751

CAS No.

1030377-48-0

DORA 42

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.

Cat. No.

A62752

CAS No.

1431472-56-8

MK-8133

MK-8133 is a selective orexin-2 receptor antagonist that inhibits orexin signaling pathways. It has demonstrated efficacy in the modulation of sleep-wake cycles, making it a valuable tool for researching insomnia and other sleep disorders. This compound can be utilized in various experimental models to investigate the role of orexin in sleep regulation and potential therapeutic interventions.