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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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