

HEK293 Cyno OX2 Stable Cell
Item | Cat# | Price |
Stable Cell Line | SNB-G-0178L | $19,800 |
Compound Testing Services | CT-001 | $1,850 per 384w plate (Up To 16 cpds Dose) |
Product Description
The Orexin Receptor 2 (OXR2), also known as HCRTR2, is a G protein-coupled receptor primarily expressed in regions such as the cerebral cortex, hippocampus, and hypothalamus. OXR2 plays important physiological roles by regulating the sleep-wake cycle, mood, learning and memory, feeding behavior, reward/addiction, and energy balance. Dysfunction of OXR2 is closely associated with sleep disorders and is involved in the pathophysiology of conditions such as insomnia, hypersomnia, depression, and narcolepsy.
Screeningbio’s HEK293/Cyno OX2 cell line overexpress HCRTR2 receptor and is designed to detect increases in intracellular Calcium flux signal in response to agonist stimulation of the receptor. Molecular Devices Calcium 6 kit can be used to detect the signal.
Product Specifications
Target Type | GPCR |
Species | Cyno |
HGNC Symbol | OX2 |
Accession Number | XM_015449292.3 |
Parental Line | HEK293 |
Lot# | See Vial |
Storage | Liquid Nitrogen |
Data
![OX2 Agonist Assay. HEK293/Cyno OX2 cells were treated with the reference agonist Orexin A. The assay was run based on FLIPR Calcium 6 Assay protocol. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 values were determined, using GraphPad Prism software.](https://static.wixstatic.com/media/cbf7de_11b4106bb038427481aaaf8048f45af5~mv2.png/v1/fill/w_75,h_75,al_c,q_85,usm_0.66_1.00_0.01,blur_2,enc_auto/cbf7de_11b4106bb038427481aaaf8048f45af5~mv2.png)
Target Background
The orexin receptor 2 (OX2, HCRTR2) is a class A G-protein-coupled receptor (GPCR) that mediates the actions of the neuropeptides orexin-A and orexin-B. OX2 is predominantly expressed in the brain, with high density in regions such as the tuberomammillary nucleus, cerebral cortex, and brainstem nuclei, while also showing peripheral expression in the pituitary, adrenal gland, and adipose tissue. Its expression profile underscores its essential role in regulating sleep-wake regulation, energy homeostasis, and autonomic functions.
Upon binding to both orexin-A and orexin-B with similar high affinity—unlike OX1 which prefers orexin-A—OX2 couples to Gq proteins, leading to phospholipase C activation and increased intracellular calcium levels, and may also signal through Gi/Go pathways. This signaling cascade influences neuronal excitability, neurotransmitter release, and synaptic plasticity. In the brain, OX2 activation is particularly critical for promoting and maintaining wakefulness, stabilizing arousal states, and regulating the sleep-wake cycle. Outside the central nervous system, OX2 has been implicated in regulating endocrine function, energy expenditure, and glucose metabolism.
Pharmacologically, OX2 has emerged as a crucial target for sleep-wake disorders. Selective OX2 receptor antagonists have been developed to treat insomnia, with compounds like seltorexant demonstrating efficacy in promoting sleep onset and maintenance. Dual OX1/OX2 antagonists such as suvorexant and daridorexant are approved medications that block both receptors to treat insomnia. More recently, OX2-selective agonists are under investigation for narcolepsy type 1 (characterized by orexin deficiency) and other conditions of pathological hypoarousal, offering potential therapeutic avenues to enhance alertness and consolidate wakefulness. With its fundamental role in stabilizing arousal states and its distinct ligand preference from OX1, OX2 continues to be a principal focus of sleep neuroscience and the development of novel neurotherapeutics.