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BMS-470539 dihydrochloride

Catalog No. T10568 CAS 2341796-82-3

BMS-470539 dihydrochloride is a highly potent and selective agonist of the melanocortin-1 receptor (MC-1R; IC50: 120 nM; EC50: 28 nM) with anti-inflammatory properties. It does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R.

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BMS-470539 dihydrochloride Chemical Structure

BMS-470539 dihydrochloride, CAS 2341796-82-3

Pack Size	Availability	Price/USD
2 mg	5 days	$ 108.00
25 mg	6-8 weeks	$ 734.00
50 mg	6-8 weeks	$ 954.00
100 mg	6-8 weeks	$ 1,740.00

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Biological Description

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Description	BMS-470539 dihydrochloride is a highly potent and selective agonist of the melanocortin-1 receptor (MC-1R; IC50: 120 nM; EC50: 28 nM) with anti-inflammatory properties. It does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R.
Targets&IC50	MC1R:120 nM, MC1R:28 nM (EC50)
In vitro	An established HBL melanoma cell line stably expresses an NF-κB luciferase reporter, allowing for the observation that TNF-α at 0.5 ng/mL incites a dose-dependent escalations in NF-κB luciferase activity. Administering BMS-470539 to these HBL-NF-κB cells leads to a dose-dependent diminution in TNF-α-induced NF-κB luciferase activity, while it remains ineffective in altering luciferase reporter activity in the absence of TNF-α induction. In nontransfected HBL cells, BMS-470539 administration shows a dose-dependent deterrence of NF-κB nuclear translocation.
In vivo	The treatment of BMS-470539 (2.05-18.47 mg/kg; i.v.; for 125 minutes; WT and MC1 receptor recessive e/e mice) inhibits cell emigration and adhesion with no effect on cell rolling. It also inhibits the tissue expression of CXCL1/CCL2 [3].

Molecular Weight	596.17
Formula	C32H42ClN5O4
CAS No.	2341796-82-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Keywords

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