Dersimelagon

SKU: orb1702360

Description

Dersimelagon (MT-7117) is an orally bioavailable, selective MC1R agonist with high affinity for human, monkey, mouse, and rat receptors. It is utilized in research to investigate skin pigmentation mechanisms, including in vitro receptor activation studies and in vivo models of dermatological conditions.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1835256-48-8
• MW: 675.75
• Purity: 98.23% (May vary between batches)
• Formula: C₃₆H₄₅F₄N₃O₅
• SMILES: C(=O)([C@@]1(F)[C@@H](CN(C1)C2CCCC2)C3=CC=C(OC)C=C3)N4C[C@@H]([C@@H](COC)C4)C5=C(C=C(C(F)(F)F)C=C5)N6CCC(C(O)=O)CC6
• Target: Melanocortin Receptor
• Solubility: DMSO:6.76 mg/mL (10 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.48 mM)

Bioactivity

• Target IC50:
  MC4R (human):32.9 nM (Ki)|MC4R (human):79.6 nM (EC50)|MC1R (rat):0.251 nM (EC50)|MC2R (human):>10000 nM (EC50)|MC1R (human):2.26 nM (Ki)|MC1R (human):8.16 nM (EC50)|MC3R (human):1420 nM (Ki)|MC5R (human):486 nM (Ki)|MC1R (mouse):1.14 nM (EC50)|MC1R (cynomolgus monkey):3.91 nM (EC50)
• In Vivo:
  METHODS: Dersimelagon (MT-7117) (0.003, 0.03, 0.3, 3 mg/kg; oral administration for 6 days) was used to observe the effect of Dersimelagon (MT-7117) on the hair of Ay/a mice. RESULTS MT-7117 induced the synthesis of eumelanin, but not pheomelanin, in the hair roots of Ay/a mice.
• In Vitro:
  METHODS: B16F1 cells were treated with Dersimelagon (MT-7117) (0, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300 pM; 3 days) to evaluate the ability of Dersimelagon (MT-7117) to induce eumelanin production. RESULTS Dersimelagon (MT-7117) increased eumelanin production in a concentration-dependent manner with an EC50 of 13 pM in B16F1 cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dersimelagon, MT7117, MT-7117, MT 7117, MelanocortinReceptor, melanocortin-1 receptor, Melanocortin Receptor

Compound Identifiers

PubChem CID

126736894