ML 00253764 hydrochloride
Cat. No. 4854
Chemical Name: 2-[2-[2-(5-Bromo-2-methoxyphenyl)et
Biological ActivityNon-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.
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.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products.
Do you know of a great paper that uses ML 00253764 hydrochloride from Tocris? If so please let us know.
View Related Products by Target
View Related Products by Product Action
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
Find multiple products by catalog number
New Products in this Area
FPR2 (lipoxin A4 receptor) agonistAmylin (rat)
Potent endogenous peptide agonist for amylin, calcitonin, CGRP and adrenomedullin receptorsCalcitonin (human)
Endogenous calcitonin receptor agonist; inhibits bone resorptionSpexin
Potent GAL2/3 agonist; exhibits anxiolytic effects in vivoMM 54
Potent apelin receptor antagonistMSG 606
Potent human MC1 receptor antagonist; also MC3 and MC5 partial agonist
One Day Symposium
March 1, 2017
Amsterdam, The Netherlands