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Orexin

Updated: 2026-07-15

Overview

Orexin (or hypocretin) is a neuropeptide produced in the hypothalamus, first identified in 1998. It exists in two forms: orexin-A (33 amino acids) and orexin-B (28 amino acids), derived from a common precursor peptide. These peptides bind to G-protein-coupled receptors OX1R and OX2R, influencing physiological processes like wakefulness, energy homeostasis, and reward-seeking behavior. Research links orexin deficiency to narcolepsy type 1, making it a key focus for sleep disorder therapeutics. Its dual role in appetite stimulation and arousal regulation has spurred pharmaceutical interest, particularly for insomnia and obesity treatments.

Physical and Chemical Properties

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Orexins are water-soluble peptides with molecular weights of 3.5–3.6 kDa. Orexin-A contains two disulfide bonds stabilizing its structure, while orexin-B is linear. Both are stable in acidic buffers but degrade under prolonged exposure to proteases or repeated freeze-thaw cycles. Their amphipathic nature allows interaction with lipid membranes, facilitating blood-brain barrier penetration in therapeutic contexts. Analytical methods like HPLC and mass spectrometry are standard for purity verification (>95% required for research).

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Main Applications

Orexin's primary application is neuroscience research, particularly studies on sleep/wake regulation and metabolic disorders. Pharmaceutical companies are developing orexin receptor antagonists (e.g., suvorexant) for insomnia and agonists for narcolepsy. In animal models, orexin supplementation restores normal sleep patterns in narcoleptic subjects. Emerging applications include addiction treatment due to its role in reward pathways, though clinical use remains experimental.

Safety and Storage

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As bioactive peptides, orexins require careful handling. Use gloves and eye protection to prevent exposure. Store lyophilized powder at -20°C in airtight containers; reconstituted solutions should be aliquoted to avoid contamination. Degradation products may exhibit unpredictable bioactivity, so avoid prolonged storage in solution. Suppliers typically provide stability data—follow recommended protocols for specific batches.

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B2B Procurement Guide

When sourcing orexins, prioritize suppliers with ISO certification and batch-specific COAs (Certificates of Analysis). Key metrics include purity (≥95%), endotoxin levels (<1 EU/μg), and peptide sequence verification via MS/MS. Bulk purchases (5+ mg) may reduce costs by 20–30%. Consider lead times (2–4 weeks for custom synthesis) and request stability data for long-term projects. Some suppliers offer conjugation services (e.g., fluorescent labels) for specialized research.

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