Biological Activity
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].
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].
In Vivo
No in vivo data are provided in the current product source. Contact us for further information.
Target
kappa opioid receptor (KOR)[1]
References & source
[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.
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.
