For research use only. Not for therapeutic Use.
ML-00253764 hydrochloride is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki and IC50 of 0.16 µM and 0.103 µM, respectively[1].
ML-00253764 displaces NDP-α-MSH binding with a mean IC50 of 0.32 μM, 0.81 μM and 2.12 μM for hMC4-R, hMC3-R and hMC5-R, respectively[1].
ML-00253764 (100 µM) decreases cAMP production induced by [NLE4,D-Phe7]-α-melanocyte stimulating hormone ([NDP]-α-MSH) by 20% in MC4R-expressing HEK293 cell membranes, but has no effect on cAMP levels in MC3R- or MC5R-expressing membranes[1].
ML-00253764 (subcutaneous injection; 3, 10, or 30 mg/kg; once daily) shows protection against tumor-induced body weight loss upon chronic, peripheral dosing in CT-26 tumor bearing BALB/c mice[1].ML-00253764 dissolves in polyethylene glycol 200/saline (1:10) in a volume of 10 mL/kg (For reference only)[1].
| Catalog Number | I011040 |
| CAS Number | 1706524-94-8 |
| Synonyms | 2-[2-[2-(5-bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole;hydrochloride |
| Molecular Formula | C18H19BrClFN2O |
| Purity | ≥95% |
| InChI | InChI=1S/C18H18BrFN2O.ClH/c1-23-17-8-6-13(19)11-12(17)5-7-14-15(3-2-4-16(14)20)18-21-9-10-22-18;/h2-4,6,8,11H,5,7,9-10H2,1H3,(H,21,22);1H |
| InChIKey | KZUMGPQDDCBFBF-UHFFFAOYSA-N |
| SMILES | COC1=C(C=C(C=C1)Br)CCC2=C(C=CC=C2F)C3=NCCN3.Cl |
| Reference | [1]. Vos TJ, et al. 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. 2004 Mar 25;47(7):1602-4. |
