BMS-470539 dihydrochloride

Product NameBMS-470539 dihydrochloride
CAS2341796-82-3
MFC32H42ClN5O4
MW596.17
EINECS
MOL File2341796-82-3.mol

Chemical Properties

storage temp.	-10 to -25°C
solubility	DMSO:63.26(Max Conc. mg/mL);100.0(Max Conc. mM) Water:63.26(Max Conc. mg/mL);100.0(Max Conc. mM)
form	A crystalline solid
color	White to off-white
Water Solubility	H2O: 2mg/mL, clear (Warmed)
SMILES	CCCC(C1(C2=CC=CC=C2)CCN(CC1)C([C@H](NC([C@@H](N)CC3=CN=CN3C)=O)CC4=CC=C(C=C4)OC)=O)=O.[2HCl]

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

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].

Biological Activity

BMS-470539 is a highly potent and selective melanocortin-1 receptor (MC-1R; MC1R) agonist (AMP stimulation EC50 = 11.6/16.2/16.8 nM using B16/HBL/CHO-MC1R; little or no potency toward MC2R, MC3R MC4R MC5R) with anti-inflammatory efficacy in mice in vivo (15-100 μmol/kg via i.v. or s.c. 0.5-1 h prior to 1 μg LPS s.c.).

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:	Wild-type (WT) and MC1 receptor recessive e/e mice induced with ischaemia-reperfusion^[3]
Dosage:	2.05 mg/kg, 6.16 mg/kg and 18.47 mg/kg
Administration:	Intravenous injection; for 125 minutes
Result:	Inhibited cell adhesion and emigration with no effect on cell rolling. Inhibited tissue expression of both CXCL1 and CCL2.

IC 50

MC1R

References

[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. DOI:10.1021/jm025600i
[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. DOI:10.1189/jlb.1204748
[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. DOI:10.1111/j.1476-5381.2010.00688.x

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