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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 | Availability | Quantity |
---|---|---|---|
1 mg | $72 | In Stock | |
5 mg | $189 | In Stock | |
10 mg | $278 | In Stock | |
25 mg | $475 | In Stock | |
50 mg | $682 | 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 | MC1R (mouse):1.14 nM (EC50), MC5R (human):486 nM (Ki), MC1R (cynomolgus monkey):3.91 nM (EC50), MC3R (human):1420 nM (Ki), MC4R (human):32.9 nM (Ki), MC4R (human):79.6 nM (EC50), MC1R (human):2.26 nM (Ki), MC1R (human):8.16 nM (EC50), MC2R (human):>10000 nM (EC50), MC1R (rat):0.251 nM (EC50) |
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] |
Alias | 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) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 6.76 mg/mL (10 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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