Dersimelagon
Based on 1 Customer Validation
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.10%
- CAS. Nr.: 1835256-48-8
- Formel: C36H45F4N3O5
- Molecular Weight:675.75
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
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) |
In Vitro
Dersimelagon (0, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300 pM; 3 days) increases eumelanin production in a concentration-dependent manner, with EC50 of 13 pM in B16F1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus monkeys[1]
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Dosage:1, 3, 10, 30 mg/kg
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Administration:P.o.; 1, 3, 10 mg/kg for 4 weeks and 30 mg/kg for 3 weeks
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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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1835256-48-8
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Appearance Solid
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Molecular Weight 675.75
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Formel C36H45F4N3O5
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Color Off-white to light yellow
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SMILES
O=C(N1C[C@H](C2=C(N3CCC(C(O)=O)CC3)C=C(C(F)(F)F)C=C2)[C@@H](COC)C1)[C@]4([C@H](C5=CC=C(OC)C=C5)CN(C6CCCC6)C4)F
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Synonyms
MT-7117
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 25 mg/mL (37.00 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4798 mL | 7.3992 mL | 14.7984 mL | 36.9959 mL |
| 5 mM | 0.2960 mL | 1.4798 mL | 2.9597 mL | 7.3992 mL | |
| 10 mM | 0.1480 mL | 0.7399 mL | 1.4798 mL | 3.6996 mL | |
| 15 mM | 0.0987 mL | 0.4933 mL | 0.9866 mL | 2.4664 mL | |
| 20 mM | 0.0740 mL | 0.3700 mL | 0.7399 mL | 1.8498 mL | |
| 25 mM | 0.0592 mL | 0.2960 mL | 0.5919 mL | 1.4798 mL | |
| 30 mM | 0.0493 mL | 0.2466 mL | 0.4933 mL | 1.2332 mL |
Dersimelagon Related Classifications
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