| Chemical Properties | Back Directory | [Boiling point ]
758.1±60.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [solubility ]
DMSO: Soluble: =10 mg/ml
Ethanol: Soluble: =10 mg/ml | [form ]
Solid | [pka]
6.88±0.60(Predicted) | [color ]
Off-white to light yellow | [InChIKey]
MUNWOYRHJPWQNE-GMFUQMJFSA-N | [SMILES]
N1(C2=CC(C(F)(F)F)=CC=C2[C@@H]2[C@@H](COC)CN(C([C@@]3(F)[C@H](C4=CC=C(OC)C=C4)CN(C4CCCC4)C3)=O)C2)CCC(C(O)=O)CC1 |
| Hazard Information | Back Directory | [Uses]
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 shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation[1][2]. | [in vivo]
Dersimelagon (0.003, 0.03, 0.3, 3 mg/kg; p.o. for 6 days) induces coat colour darkening in Ay/a mice in 0.3 and 3 mg/kg[1].
Dersimelagon (0.03, 0.3, 3 mg/kg; p.o.; single administration) upregulates the expression of Tyr, Trp1 and Dct of Ay/a mice at 24, 48 and 72 h in the 3 mg/kg[1].
Dersimelagon (1, 3, 10 mg/kg for 4 weeks and 30 mg/kg for 3 weeks; p.o.) induces pigmentation in a dose-dependent manner, and it is reverses after cessation of administration in cynomolgus monkeys[1].
| Animal Model: | Cynomolgus monkeys[1] | | Dosage: | 1, 3, 10, 30 mg/kg | | Administration: | P.o.; 1, 3, 10 mg/kg for 4 weeks and 30 mg/kg for 3 weeks | | Result: | Induced pigmentation in a dose-dependent manner.
Minimum pigmentation effective dose was 1 mg/kg.
Pigmentation diminished 4 weeks after cessation of treatment in the 1, 3 and 10 mg/kg groups and 16 weeks after cessation in the 30 mg/kg group.
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| [IC 50]
hMC1R: 2.26 nM (Ki); hMC4R: 32.9 nM (Ki); hMC5R: 486 nM (Ki); hMC3R: 1420 nM (Ki); hMC1R: 8.16 nM (EC50); hMC4R: 79.6 nM (EC50); hMC2R: >10000 nM (EC50); rMC1R: 0.251 nM (EC50); mMC1R: 1.14 nM (EC50); cmMC1R: 3.91 nM (EC50) | [References]
[1] T. Suzuki, et al. Melanogenic effect of dersimelagon (MT-7117), a novel oral melanocortin 1 receptor agonist. Skin Health Dis. 2022; 2(1):e78.
[2] Erwin AL, et al. Porphyrias in the Age of Targeted Therapies. Diagnostics (Basel). 2021;11(10):1795. Published 2021 Sep 29. DOI:10.3390/diagnostics11101795 |
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| Company Name: |
cjbscvictory
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| Telephone: |
13348960310 13348960310 |
| Website: |
www.weikeqi-biotech.com/ |
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