U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 12021 - 12030 of 13311 results

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



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.

Showing 12021 - 12030 of 13311 results