BMS-470539 dihydrochloride

TargetMol
Product Code: TAR-T10568
Supplier: TargetMol
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TAR-T10568-50mg50mg£837.00
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TAR-T10568-100mg100mg£1,468.00
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Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

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Further Information

Bioactivity:
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.
CAS:
2341796-82-3
Formula:
C32H43Cl2N5O4
Molecular Weight:
632.62
Purity:
0.98
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

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. 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.