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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

Images & Validation

Key Properties

CAS Number1835256-48-8
MW675.75
Purity97.35% (May vary between batches)
FormulaC36H45F4N3O5
SMILESC(=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
TargetMelanocortin Receptor
SolubilityDMSO: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-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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

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Key Properties

No computed properties available.

Protocol Information

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1 mg
$ 120.00
5 mg
$ 230.00
10 mg
$ 320.00
25 mg
$ 520.00
50 mg
$ 730.00
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