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Difelikefalin (CR845)

Names

[ CAS No. ]:
1024828-77-0

[ Name ]:
Difelikefalin (CR845)

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C36H53N7O6

[ Molecular Weight ]:
679.84900

[ Exact Mass ]:
679.40600

[ PSA ]:
222.97000

[ LogP ]:
4.04460

Related Compounds