Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 1-[2-[(3S,4R)-1-[[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)-3-pyrrolidinyl]carbonyl]-4-(methoxymethyl)-3-pyrrolidinyl]-5-(trifluoromethyl)phenyl]-4-piperidinecarboxylic acid
Purity: ≥98%
Formula Markup: C36H45F4N3O5
Formula Weight: 675.8
CAS Number: 1835256-48-8
Notes: Dersimelagon is an agonist of melanocortin receptor 1 (MC1R).{69923} It selectively induces cAMP accumulation in HEK293 cells expressing human MC1R (EC50 = 8.16 nM) over HEK293 cells expressing human MC2R (EC50 = >10,000 nM) but also induces cAMP accumulation in HEK293 cells expressing human MC4R (EC50 = 79.6 nM). Dersimelagon increases melanin levels in B16-F1 melanocytes (EC50 = 13 pM). It increases eumelanin levels in the hair roots of, and induces coat darkening in, mice when administered at doses of 0.3 or 3 mg/kg per day. Dersimelagon (3 mg/kg per day) also decreases bleomycin-induced increases in skin thickness, skin levels of collagen, dermal levels of myofibroblasts, lung weight, and serum levels of pulmonary surfactant-associated protein D (PSP-D), adiponectin, matrix metalloproteinase-2 (Mmp-2), Mmp-3, P-selectin, Tnf receptor 1 (Tnfr1), and Tnfr2 in a mouse model of bleomycin-induced systemic sclerosis.{69924}
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