2. GPCR/G Protein Neuronal Signaling
  3. Melanocortin Receptor
  4. Resomelagon

Resomelagon  (Synonyms: AP1189)

Cat. No.: HY-147301 Purity: 99.63%
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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.

For research use only. We do not sell to patients.

Resomelagon Chemical Structure

Resomelagon Chemical Structure

CAS No. : 1809420-71-0

Size Price Stock Quantity
5 mg USD 260 In-stock
10 mg USD 380 In-stock
25 mg USD 800 In-stock
50 mg USD 1280 In-stock
100 mg USD 2100 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Resomelagon:

Resomelagon Related Antibodies

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  • Purity & Documentation

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Description

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[1][2].

IC50 & Target

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.

Resomelagon Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293A cells
Concentration: 0-1000 μM
Incubation Time: 8 minutes
Result: Increased the expression of ERK1/2 phosphorylation in a dose-dependent manner.
In Vivo

Resomelagon (0-10 mg/kg; i.p., i.v. and p.o.; for 24 h; male C57BL/6J wild-type (WT) and BALB/c mice) promotes resolution of acute inflammation in vivo[1].
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.

Animal Model: Male C57BL/6J wild-type (WT) and BALB/c mice[1]
Dosage: 0, 0.1, 1 and 10 mg/kg
Administration: Oral administration, intraperitoneal injection and intravenous injection; for 24 hours
Result: Inhibited neutrophil and monocyte infiltration in a dose-dependent manner.
Animal Model: Male C57BL/6J wild-type (WT) and BALB/c mice[1]
Dosage: 25 and 50 mg/kg
Administration: Oral administration; daily; for 8 days
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%).
Clinical Trial
Molecular Weight

298.30

Formula

C14H14N6O2
CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

N=C(N)N/N=C/C=C/C1=CC=CN1C2=C(C=CC=C2)[N+]([O-])=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3523 mL 16.7617 mL 33.5233 mL
5 mM 0.6705 mL 3.3523 mL 6.7047 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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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Resomelagon Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Resomelagon1809420-71-0AP1189AP 1189AP-1189Melanocortin ReceptorMC ReceptorERK1/2 phosphorylationCa2+anti-inflammatoryobesitychronic inflammationInhibitorinhibitorinhibit

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