ML 00253764 hydrochloride

Cat. No. 4854

ML 00253764 hydrochloride C18H18BrFN2O.HCl [1706524-94-8]

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Chemical Name: 2-[2-[2-(5-Bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-2-1H-imidazole hydrochloride

Biological Activity

Non-peptide, melanocortin MC4 receptor antagonist (IC50 values are 320, 810 and 2120 nM for MC4, MC3 and MC5 receptors respectively). Decreases cAMP accumulation in HEK-293 cells expressing the MC4 receptor. Increases food intake and reduces loss of lean body mass in tumor bearing mice. Brain penetrant.

Technical Data

M.Wt:
413.71
Formula:
C18H18BrFN2O.HCl
Solubility:
Soluble to 10 mM in water and to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
1706524-94-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Nicholson et al (2006) Peripheral administration of a melanocortin 4-receptor inverse agonist prevents loss of lean body mass in tumor-bearing mice. J.Pharmacol.Exp.Ther. 317 771. PMID: 16436498.

Tucci et al (2005) Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines. Bioorg.Med.Chem.Lett. 15 4389. PMID: 16098742.

Vos et al (2004) Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model. J.Med.Chem. 47 1602. PMID: 15027849.

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Keywords: ML 00253764 hydrochloride, supplier, ML00253764, hydrochloride, non-peptide, inverse, agonists, antagonists, melanocortin, MC4, receptors, cachexia, in, vivo, brain, penetrant, Tocris Bioscience, Melanocortin (MC) Receptor Antagonist products

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