LIH383 is a peptide agonist specifically designed to activate the chemokine (C-X-C motif) receptor 7 (CXCR7), which functions both as a chemokine and an opioid peptide scavenger receptor. Demonstrating a high selectivity, LIH383 activates CXCR7 with an effective concentration (EC50) of 0.61 nM, showing significantly lower affinity towards µ-, delta-, and kappa-opioid receptors, as well as the nociceptin opioid peptide (NOP) receptor, even at concentrations of 3 µM in beta-arrestin recruitment assays. Furthermore, at a concentration of 3 µM, LIH383 effectively inhibits the uptake of opioid peptides by CXCR7, a process normally induced by dynorphin A, a non-selective opioid receptor agonist, in U87-ACKR3 cells.
Molekulargewicht:
997.22
Formel:
C45H72N16O8S.XCF3COOH
Target-Kategorie:
CXCR
T83709
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