描述
Difelikefalin (also known as CR845) is a peripherally restricted and selective kappa opioid receptor agonist peptide. Unlike traditional opioids, Difelikefalin does not significantly cross the blood-brain barrier, minimizing central nervous system side effects. It acts primarily on peripheral KORs, modulating pain signals and itch responses in experimental models. This unique mechanism makes Difelikefalin a valuable tool in preclinical research for pain management, especially in conditions like chronic pain, neuropathic pain, and pruritus.
Product Specifications
Parameter | Details |
---|---|
Product Name | Difelikefalin |
Synonyms | CR845 |
CAS Number | 1024828-77-0 |
Purity | 99.98% (HPLC) |
Molecular Formula | C44H66N12O12 |
Molecular Weight | Approx. 946.06 Da |
Appearance | White to off-white lyophilized powder |
Solubility | Soluble in water and aqueous buffers |
Storage | Store at –20°C, protect from light and moisture |
GMP Compliance | Yes |
Intended Use | Laboratory research only |
Mechanism of Action & Research Applications
Difelikefalin selectively activates kappa opioid receptors located on peripheral sensory neurons and immune cells. Its peripheral restriction avoids typical opioid-related central nervous system effects such as sedation or addiction potential. This selective action modulates peripheral pain signals and inhibits itch pathways, making it a potent agent in the study of chronic pain, neuropathic pain, and pruritus mechanisms.
Research uses include:
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Investigating peripheral analgesic pathways
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Studying mechanisms of chronic and neuropathic pain
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Exploring therapeutic targets for pruritus
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Evaluating opioid receptor pharmacology with minimized CNS effects
Side Effects (For Research Context Only)
In experimental settings, Difelikefalin may cause transient changes in nociceptive signaling or immune cell activity. No central nervous system-related adverse effects are expected due to its peripheral action.
Disclaimer
is intended solely for laboratory research use and is not approved for clinical or therapeutic applications.
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