BMS 470539 dihydrochloride

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Cat.No. 4053 - BMS 470539 dihydrochloride | C32H41N5O4.2HCl | CAS No. 2341796-82-3
Description: Potent, selective MC1 receptor agonist
Chemical Name: 1-[1-(3-Methyl-L-histidyl-O-methyl-D-tyrosyl)-4-phenyl-4-piperidinyl]-1-butanone dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (3)

Biological Activity

Potent, selective melanocortin MC1 receptor agonist (IC50 = 120 nM). Exhibits anti-inflammatory properties following ischemia-reperfusion in the vasculature. Inhibits leukocyte trafficking.

Compound Libraries

BMS 470539 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 632.62
Formula C32H41N5O4.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 2341796-82-3
PubChem ID 60210130
InChI Key DUAOBJHRUKFKIH-YDVFRNEYSA-N
Smiles O=C(N2CCC(C(CCC)=O)(C4=CC=CC=C4)CC2)[C@H](NC([C@@H](N)CC3=CN=CN3C)=O)CC1=CC=C(OC)C=C1.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 63.26 100
DMSO 63.26 100

Preparing Stock Solutions

The following data is based on the product molecular weight 632.62. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.58 mL 7.9 mL 15.81 mL
5 mM 0.32 mL 1.58 mL 3.16 mL
10 mM 0.16 mL 0.79 mL 1.58 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

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References

References are publications that support the biological activity of the product.

Herpin et al (2003) Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties. J.Med.Chem. 46 1123 PMID: 12646021

Leoni et al (2010) The melanocortin MC1 receptor agonist BMS-470539 inhibits leukocyte trafficking in the inflamed vasculature. Br.J.Pharmacol. 160 171 PMID: 20331604

Kang (2006) A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice. J.Leukoc.Biol. 80 897 PMID: 16888084


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View all Melanocortin (MC) Receptor Agonists

Keywords: BMS 470539 dihydrochloride, BMS 470539 dihydrochloride supplier, BMS470539, melanocortin, agonist, MC1, agonists, anti-inflammatory, 457893-92-4, Melanocortin, Receptors, 4053, Tocris Bioscience

1 Citation for BMS 470539 dihydrochloride

Citations are publications that use Tocris products. Selected citations for BMS 470539 dihydrochloride include:

Jain et al (2018) Melanotan II causes hypothermia in mice by activation of mast cells and stimulation of histamine 1 receptors. Am J Physiol Endocrinol Metab 315 E357 PMID: 29812984


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Literature in this Area

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