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Chemical Structure : ML00253764 hydrochloride
Catalog No.: PC-61574Not 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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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; decreases cAMP accumulation in HEK-293 cells expressing the MC4 receptor, increases food intake and effectively reduces tumor-induced weight loss in mouse model; 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.
| M.Wt | 413.71 | |
| Formula | C18H18BrFN2O.HCl | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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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