ML 00253764 hydrochloride

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Cat.No. 4854 - ML 00253764 hydrochloride | C18H18BrFN2O.HCl | CAS No. 1706524-94-8
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)
Datasheet
Citations
Literature

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
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1706524-94-8
PubChem ID 90488979
InChI Key KZUMGPQDDCBFBF-UHFFFAOYSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 413.71. Batch specific molecular weights may vary from batch to batch due to solvent 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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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Keywords: ML00253764 hydrochloride non-peptide inverse agonists antagonists melanocortin MC4 receptors cachexia in vivo brain penetrant Melanocortin Receptors

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