ML 00253764 hydrochloride

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Description: Melanocortin MC4 receptor antagonist; brain penetrant
Chemical Name: 2-[2-[2-(5-Bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-2-1H-imidazole hydrochloride
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for ML 00253764 hydrochloride

ML 00253764 hydrochloride is a 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.

Compound Libraries for ML 00253764 hydrochloride

ML 00253764 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for ML 00253764 hydrochloride

M. Wt 413.71
Formula C18H18BrFN2O.HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1706524-94-8
PubChem ID 90488979
Smiles BrC1=CC(CCC2=C(F)C=CC=C2C3=NCCN3)=C(OC)C=C1.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 for ML 00253764 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 4.14 10
DMSO 41.37 100

Preparing Stock Solutions for ML 00253764 hydrochloride

The following data is based on the product molecular weight 413.71. 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 2.42 mL 12.09 mL 24.17 mL
5 mM 0.48 mL 2.42 mL 4.83 mL
10 mM 0.24 mL 1.21 mL 2.42 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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Product Datasheets for ML 00253764 hydrochloride

Certificate of Analysis / Product Datasheet
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References for ML 00253764 hydrochloride

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

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

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

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

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Citations for ML 00253764 hydrochloride

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Literature in this Area

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Peptides Involved in Appetite Modulation Scientific Review

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.