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首页-小分子抑制剂&激动剂-GPCR-Melanocortin Receptor-Dersimelagon
Dersimelagon

Chemical Structure : Dersimelagon

CAS No.: 1835256-48-8

Dersimelagon (MT-7117, MT7117)

货号: PC-35446Not For Human Use, Lab Use Only.

Dersimelagon (MT-7117) is an orally bioavailable selective, non-peptide melanocortin-1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human, cynomolgus monkey, mouse and rat MC1R, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Dersimelagon (MT-7117) is an orally bioavailable selective, non-peptide melanocortin-1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human, cynomolgus monkey, mouse and rat MC1R, respectively.
Dersimelagon (MT-7117) shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively.
Dersimelagon (MT-7117) increases eumelanin production in a concentration-dependent manner, with EC50 of 13 pM in B16F1 cells.

 

物理化学性质&存储条件

分子量 675.766
分子式 C36H45F4N3O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-{2-[(3S,4R)-1-[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidine-3-carbonyl]-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylic acid

参考文献

1.  Angelika L Erwin, et al. Diagnostics (Basel). 2021 Sep 29;11(10):1795.
2. T. Suzuki, et al. Skin Health Dis. 2022; 2(1):e78.

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