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Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14, and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m), and rat (r) MC1R, respectively. Dersimelagon exhibits good affinity for hMC1R and hMC4R, with Ki values of 2.26 and 32.9 nM, respectively. Dersimelagon can be used in the study of skin pigmentation[1].

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $72 | In Stock | In Stock | |
| 5 mg | $189 | In Stock | In Stock | |
| 10 mg | $278 | In Stock | In Stock | |
| 25 mg | $475 | In Stock | In Stock | |
| 50 mg | $682 | In Stock | In Stock |
| Description | Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14, and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m), and rat (r) MC1R, respectively. Dersimelagon exhibits good affinity for hMC1R and hMC4R, with Ki values of 2.26 and 32.9 nM, respectively. Dersimelagon can be used in the study of skin pigmentation[1]. |
| Targets&IC50 | MC4R (human):79.6 nM (EC50), MC1R (rat):0.251 nM (EC50), MC5R (human):486 nM (Ki), MC1R (human):8.16 nM (EC50), MC1R (cynomolgus monkey):3.91 nM (EC50), MC2R (human):>10000 nM (EC50), MC3R (human):1420 nM (Ki), MC1R (mouse):1.14 nM (EC50), MC1R (human):2.26 nM (Ki), MC4R (human):32.9 nM (Ki) |
| 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. [1] |
| 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. [1] |
| Synonyms | MT-7117 |
| Molecular Weight | 675.75 |
| Formula | C36H45F4N3O5 |
| Cas No. | 1835256-48-8 |
| 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 |
| Relative Density. | 1.33 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 6.76 mg/mL (10 mM), Sonication is recommended. | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.48 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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