Dersimelagon
- Product Name
- 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
- Formula Weight
- 675.75
- MOL File
- 1835256-48-8.mol
Dersimelagon Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
Dersimelagon Chemical Properties,Usage,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
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View Lastest Price from Dersimelagon manufacturers
- Product
- Dersimelagon 1835256-48-8
- Price
- US $1900.00/g
- Min. Order
- 0.1g
- Purity
- 98+
- Supply Ability
- 100g
- Release date
- 2024-01-25