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Search results for l root_names_stdName in Standardized Name (approximate match)
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
BMS-470539 2 HCL (BMS-470539) is a potent, specific MC1R ligand. The
affinity of this molecule, as determined by [125I]NDP-MSH
competition binding experiments, was in the nanomolar
range (IC50 120 nM). BMS-470539 is a
potent, full agonist of recombinant human MC-1R, stably expressed
in CHO cells, with an EC50 of 16.8 nM and an intrinsic
activity of 88% in a cAMP accumulation assay. BMS-470539 exhibits anti-inflammatory properties following ischemia-reperfusion in the vasculature. BMS-470539 inhibits leukocyte trafficking. In mice, BMS-470539 inhibits lipopolysaccharide (LPS)-induced systemic tumour necrosis factor (TNF) release and LPS-induced leucocyte migration into the lung.