| Description | Dersimelagon (MT-7117) is an orally active, selective agonist for the melanocortin 1 receptor (MC1R), demonstrating EC50 values of 8.16 nM (h), 3.91 nM (cm), 1.14 nM (m), and 0.251 nM (r) across species such as human, cynomolgus monkey, mouse, and rat, respectively. It exhibits strong affinity for human MC1R and MC4R, with Ki values of 2.26 nM and 32.9 nM, respectively. This compound is applied in the study of skin pigmentation. |
| In vitro | Dersimelagon (0、0.03、0.1、0.3、1、3、10、30、100、300 pM；3天) 以浓度依赖方式增加B16F1细胞中的黑色素生成，EC50值为13 pM[1]。 |
| In vivo | Dersimelagon（0.003、0.03、0.3、3 mg/kg；口服6天）在0.3及3 mg/kg[1]剂量下，能够引起Ay/a小鼠毛色变深。 |
| Target activity | MC2R (human):>10000 nM (EC50), MC1R (human):8.16 nM (EC50), MC1R (human):2.26 nM (Ki), MC1R (rat):0.251 nM (EC50), MC4R (human):79.6 nM (EC50), MC4R (human):32.9 nM (Ki), MC3R (human):1420 nM (Ki), MC1R (cynomolgus monkey):3.91 nM (EC50), MC5R (human):486 nM (Ki), MC1R (mouse):1.14 nM (EC50) |
| Synonyms | MT-7117 |
| molecular weight | 675.75 |
| Molecular formula | C36H45F4N3O5 |
| CAS | 1835256-48-8 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 6.76 mg/mL (10 mM), Sonication is recommended. |
| References | 1. T. Suzuki, et al. Melanogenic effect of dersimelagon (MT-7117), a novel oral melanocortin 1 receptor agonist. Skin Health Dis. 2022; 2(1):e78. 2. Erwin AL, et al. Porphyrias in the Age of Targeted Therapies. Diagnostics (Basel). 2021;11(10):1795. Published 2021 Sep 29 |