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ML00253764

Chemical Structure : ML00253764

CAS No.: 681847-92-7

ML00253764 (ML 00253764)

Catalog No.: PC-61573Not For Human Use, Lab Use Only.

ML00253764 is a non-peptide, brain penetrant melanocortin MC4 receptor (MC4R) antagonist with IC50 of 0.32, 0.81 and 2.12 uM for MC4, MC3 and MC5 receptors, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ML00253764 is a non-peptide, brain penetrant melanocortin MC4 receptor (MC4R) antagonist with IC50 of 0.32, 0.81 and 2.12 uM for MC4, MC3 and MC5 receptors, respectively.
ML00253764 decreases cAMP accumulation in HEK-293 cells expressing the MC4 receptor, increases food intake and effectively reduces tumor-induced weight loss in mouse model.
ML00253764 exhibits an antiproliferative and proapoptotic activity through the inhibition of the phosphorylation of ERK1/2 and Akt in glioblastoma cell, also shows highly synergistic effect combined with temozolomide both in vitro and in vivo.

Physicochemical Properties

M.Wt 377.257
Formula C18H18BrFN2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole

References

1. Vos TJ, et al. J Med Chem. 2004 Mar 25;47(7):1602-4.

2. Nicholson JR, et al. J Pharmacol Exp Ther. 2006 May;317(2):771-7.

3. Vaglini F, et al. Mol Neurobiol. 2017 Aug 8. doi: 10.1007/s12035-017-0702-4.

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