1024828-77-0

1024828-77-0 structure

Name: Difelikefalin (CR845)
Chemical Name: Difelikefalin
CAS Number: 1024828-77-0
Molecular Formula: C₃₆H₅₃N₇O₆
Molecular Weight: 679.84900
Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
Create Date: 2018-03-03 04:24:59
Modify Date: 2024-01-09 23:20:02
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease[1][2].

Name	Difelikefalin
Synonyms	CR845 FE-202845 D-Phe-D-Phe-D-Leu-D-Lys-[γ-(4-N-piperidinyl)amino carboxylic acid] 4-Piperidinecarboxylic acid, N1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-amino- N1-(D-Phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-amino-4-piperidinecarboxylic acid 1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-aminopiperidine-4-carboxylic acid

Description	Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease[1][2].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Opioid Receptor Signaling Pathways >> Neuronal Signaling >> Opioid Receptor Research Areas >> Neurological Disease
Target	kappa opioid receptor (KOR)[1]
In Vitro	Difelikefalin (CR-845; FE-202845) does not penetrate the blood-brain barrier. Difelikefalin does not bind to mu opioid receptors or any other receptors beside KORs[1].
References	[1]. Steven Fishbane, et al. Randomized Controlled Trial of Difelikefalin for Chronic Pruritus in Hemodialysis Patients. Kidney Int Rep. 2020 Jan 28;5(5):600-610. [2]. Steven Fishbane, et al. A Phase 3 Trial of Difelikefalin in Hemodialysis Patients With Pruritus. N Engl J Med. 2020 Jan 16;382(3):222-232.