BMS-470539 (dihydrochloride)

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].

Product Specifications

CAS Number

[2341796-82-3]

UNSPSC

12352005

Target

Melanocortin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/bms-470539-dihydrochloride.html

Purity

99.85

Solubility

DMSO : ≥ 125 mg/mL|H2O : ≥ 100 mg/mL

Smiles

CCCC(C1(C2=CC=CC=C2)CCN(C([C@@H](CC3=CC=C(C=C3)OC)NC([C@H](CC4=CN=CN4C)N)=O)=O)CC1)=O.Cl.Cl

Molecular Formula

C32H43Cl2N5O4

Molecular Weight

632.62

References & Citations

[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.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

MC1R

Available Sizes

Curated Selection

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