Resomelagon
Based on 1 Customer Validation
Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.79%
- CAS No.: 1809420-71-0
- Formule: C14H14N6O2
- Masse moléculaire:298.30
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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MC1R |
MC3R |
In Vitro
Resomelagon (0-1000 μM; 8 min; HEK293A cells) promotes melanocortin signal transduction through ERK1/2 phosphorylation and Ca2+ mobilization[1].
Resomelagon (1 nM; 30 min; peritoneal macrophages) has anti-inflammatory activity and inhibits TNF-α release and efferocytosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293A cells
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Concentration:0-1000 μM
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Incubation Time:8 minutes
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Result:Increased the expression of ERK1/2 phosphorylation in a dose-dependent manner.
In Vivo
Resomelagon (25-50 mg/kg; p.o.; daily, for 8 d; male C57BL/6J wild-type (WT) and BALB/c mice) reduces arthritis in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J wild-type (WT) and BALB/c mice[1]
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Dosage:0, 0.1, 1 and 10 mg/kg
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Administration:Oral administration, intraperitoneal injection and intravenous injection; for 24 hours
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Result:Inhibited neutrophil and monocyte infiltration in a dose-dependent manner.
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Animal Model:Male C57BL/6J wild-type (WT) and BALB/c mice[1]
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Dosage:25 and 50 mg/kg
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Administration:Oral administration; daily; for 8 days
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Result:Reduced all signs of arthritis measured, including clinical score (-42%), paw swelling (-87%), proportion of animals with all four paws affected (-50%), and the severity of the inflammation (-70%).
Chemical Information
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CAS No. 1809420-71-0
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Appearance Solid
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Masse moléculaire 298.30
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Formule C14H14N6O2
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Color Light brown to brown
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SMILES
N=C(N)N/N=C/C=C/C1=CC=CN1C2=C(C=CC=C2)[N+]([O-])=O
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Synonyms
AP1189
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (335.23 mM; Need ultrasonic; 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: 5 mg/mL (16.76 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (16.76 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Montero-Melendez T, et, al. Biased agonism as a novel strategy to harness the proresolving properties of melanocortin receptors without eliciting melanogenic effects. J Immunol. 2015 Apr 1;194(7):3381-8. [Content Brief]
[2]. WHO Drug Information. International Nonproprietary Names for Pharmaceutical
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 (protect from light). 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 |
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| DMSO | 1 mM | 3.3523 mL | 16.7617 mL | 33.5233 mL | 83.8083 mL |
| 5 mM | 0.6705 mL | 3.3523 mL | 6.7047 mL | 16.7617 mL | |
| 10 mM | 0.3352 mL | 1.6762 mL | 3.3523 mL | 8.3808 mL | |
| 15 mM | 0.2235 mL | 1.1174 mL | 2.2349 mL | 5.5872 mL | |
| 20 mM | 0.1676 mL | 0.8381 mL | 1.6762 mL | 4.1904 mL | |
| 25 mM | 0.1341 mL | 0.6705 mL | 1.3409 mL | 3.3523 mL | |
| 30 mM | 0.1117 mL | 0.5587 mL | 1.1174 mL | 2.7936 mL | |
| 40 mM | 0.0838 mL | 0.4190 mL | 0.8381 mL | 2.0952 mL | |
| 50 mM | 0.0670 mL | 0.3352 mL | 0.6705 mL | 1.6762 mL | |
| 60 mM | 0.0559 mL | 0.2794 mL | 0.5587 mL | 1.3968 mL | |
| 80 mM | 0.0419 mL | 0.2095 mL | 0.4190 mL | 1.0476 mL | |
| 100 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL | 0.8381 mL |
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