Cas No.: | 681847-92-7 |
Chemical Name: | 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole |
Synonyms: | ML 00253764 |
Formula: | C18H18BrFN2O |
M.Wt: | 377.257 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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. |