|Description||Difelikefalin is an analgesic opioid peptide acting as a peripherally specific, highly selective agonist of the κ-opioid receptor (KOR). It acts as an analgesic by activating KORs on peripheral nerve terminals and KORs expressed by certain immune system cells. It may be useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. It is under development by Cara Therapeutics as an intravenous agent for the treatment of postoperative pain. It lacks the central side effects due to its peripheral selectivity. It is also being investigated for the treatment of pruritus (itching). It has completed phase II clinical trials for postoperative pain and has demonstrated significant and "robust" clinical efficacy, along with being safe and well-tolerated. It is also in phase II clinical trials for uremic pruritus in hemodialysis patients.|
|Synonyms||CR845;CR-845;MR-13A-9;1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-aminopiperidine-4-carboxylic acid;4-Amino-1-[(2R)-6-amino-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid|
|Solubility||10 mM in DMSO|
|Application||Difelikefalin may be useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. It is used as an intravenous agent for the treatment of postoperative pain. It is also being investigated for the treatment of pruritus (itching).|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
|Boiling Point||1005.5±65.0 °C | Condition: Press: 760 Torr|
|Density||1.214±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr|
|Current Developer||Difelikefalin is under development by Cara Therapeutics. It has completed phase II clinical trials for postoperative pain. It is also in phase II clinical trials for uremic pruritus in hemodialysis patients.|
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