Dersimelagon
- CAS No.
- 1835256-48-8
- Chemical Name:
- Dersimelagon
- Synonyms
- Dersimelagon;Dersimelagon, 10 mM in DMSO;1-{2-[(3S,4R)-1-[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidine-3-carbonyl]-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylic acid;4-Piperidinecarboxylic acid, 1-[2-[(3S,4R)-1-[[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)-3-pyrrolidinyl]carbonyl]-4-(methoxymethyl)-3-pyrrolidinyl]-5-(trifluoromethyl)phenyl]-
- CBNumber:
- CB24667818
- Molecular Formula:
- C36H45F4N3O5
- Molecular Weight:
- 675.75
- MDL Number:
- MOL File:
- 1835256-48-8.mol
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 |
FDA UNII | 1CWH5SV4G2 |
NCI Drug Dictionary | dersimelagon |
Dersimelagon Chemical Properties,Uses,Production
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. |
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
[3] MASAHIRO KONDO. Dersimelagon, a novel oral melanocortin 1 receptor agonist, demonstrates disease-modifying effects in preclinical models of systemic sclerosis.[J]. Arthritis Research & Therapy, 2022: 210. DOI: 10.1186/s13075-022-02899-3
Dersimelagon Preparation Products And Raw materials
Raw materials
Preparation Products
Dersimelagon Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32432 | 58 |
Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 5221 | 58 |
Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | 024-024-024-88590548 18341751992 | 757984502@qq.com | China | 941 | 58 |
Bide Pharmatech Ltd. | 400-164-7117 13681763483 | product02@bidepharm.com | China | 42446 | 60 |
Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4669 | 55 | |
Shanghai Han-Xiang Chemical Co., Ltd. | 15971444841 | amber@biochempartner.com | China | 3061 | 58 |
Guangzhou Younan Technology Co., Ltd | 020-82000279 18988968278 | YN_research@163.com | China | 3003 | 58 |
Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd | 15317229551 | 15151849396@163.com | China | 997 | 58 |
View Lastest Price from Dersimelagon manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
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2025-09-30 | Dersimelagon
1835256-48-8
|
US $72.00-278.00 / mg | 98.23% | 10g | TargetMol Chemicals Inc. | ||
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2024-01-25 | Dersimelagon
1835256-48-8
|
US $1900.00 / g | 0.1g | 98+ | 100g | Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd |
-
- Dersimelagon
1835256-48-8
- US $72.00-278.00 / mg
- 98.23%
- TargetMol Chemicals Inc.
-
- Dersimelagon
1835256-48-8
- US $1900.00 / g
- 98+
- Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd