BMS-470539 dihydrochloride_product_DataBase

Bioactivity	BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. BMS-470539 dihydrochloride does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. BMS-470539 dihydrochloride has potently anti-inflammatory properties[1][2][3].
Target	IC50: 120 nM (Melanocortin-1 receptor); EC50: 28 nM (Melanocortin-1 receptor)
Invitro	An HBL melanoma cell line is established that stably expresses a NF-κB luciferase reporter. In these cells, 0.5 ng/mL TNF-α induces a dose-dependent increase in NF-κB luciferase activity. Treatment of HBL-NF-κB cells with BMS-470539 elicits a dose-dependent, statistically significant reduction in TNF-α-stimulated NF-κB luciferase activity. BMS-470539 has no effect on luciferase reporter activity in the absence of TNF-α stimulation. In nontransfected HBL cells, treatment with BMS-470539 results in a dose-dependent inhibition of NF-B nuclear translocation[2].
In Vivo	BMS-470539 (2.05-18.47 mg/kg; intravenous injection; for 125 minutes; WT and MC1 receptor recessive e/e mice) treatment inhibits cell adhesion and emigration with no effect on cell rolling. And also inhibits the tissue expression of both CXCL1 and CCL2[3]. Animal Model:
Name	BMS-470539 dihydrochloride
CAS	2341796-82-3
Formula	C32H43Cl2N5O4
Molar Mass	632.62
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Herpin TF, et al. Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties. J Med Chem. 2003 Mar 27;46(7):1123-6. [2]. Kang L, et al. A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice. J Leukoc Biol. 2006 Oct;80(4):897-904. Epub 2006 Aug 3. [3]. Leoni G, et al. The melanocortin MC(1) receptor agonist BMS-470539 inhibits leucocyte trafficking in the inflamed vasculature. Br J Pharmacol. 2010 May;160(1):171-80.

PeptideDB

BMS-470539 dihydrochloride

CAS: 2341796-82-3 F: C32H43Cl2N5O4 W: 632.62