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Dersimelagon

Name: Dersimelagon
Brand: TargetMol
SKU: T25310
Price: 72 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T25310Cas No. 1835256-48-8

Alias MT-7117

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 exhibits good affinity for hMC1R and hMC4R, with Ki values of 2.26 and 32.9 nM, respectively. Dersimelagon can be used in the study of skin pigmentation[1].

Dersimelagon

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Purity: 98.23%

Catalog No. T25310Alias MT-7117Cas No. 1835256-48-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$72	In Stock	In Stock
5 mg	$189	In Stock	In Stock
10 mg	$278	In Stock	In Stock
25 mg	$475	In Stock	In Stock
50 mg	$682	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.23%

Appearance:Solid

Color:White to Yellow

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	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 exhibits good affinity for hMC1R and hMC4R, with Ki values of 2.26 and 32.9 nM, respectively. Dersimelagon can be used in the study of skin pigmentation[1].
Targets&IC50	MC5R (human):486 nM (Ki), MC1R (mouse):1.14 nM (EC50), MC4R (human):32.9 nM (Ki), MC4R (human):79.6 nM (EC50), MC3R (human):1420 nM (Ki), MC1R (cynomolgus monkey):3.91 nM (EC50), MC2R (human):>10000 nM (EC50), MC1R (human):2.26 nM (Ki), MC1R (human):8.16 nM (EC50), MC1R (rat):0.251 nM (EC50)
In vitro	METHODS: B16F1 cells were treated with Dersimelagon (MT-7117) (0, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300 pM; 3 days) to evaluate the ability of Dersimelagon (MT-7117) to induce eumelanin production. RESULTS Dersimelagon (MT-7117) increased eumelanin production in a concentration-dependent manner with an EC50 of 13 pM in B16F1 cells. [1]
In vivo	METHODS: Dersimelagon (MT-7117) (0.003, 0.03, 0.3, 3 mg/kg; oral administration for 6 days) was used to observe the effect of Dersimelagon (MT-7117) on the hair of Ay/a mice. RESULTS MT-7117 induced the synthesis of eumelanin, but not pheomelanin, in the hair roots of Ay/a mice. [1]
Synonyms	MT-7117

Chemical Properties

Molecular Weight	675.75
Formula	C₃₆H₄₅F₄N₃O₅
Cas No.	1835256-48-8
Smiles	C(=O)([C@@]1(F)[C@@H](CN(C1)C2CCCC2)C3=CC=C(OC)C=C3)N4C[C@@H]([C@@H](COC)C4)C5=C(C=C(C(F)(F)F)C=C5)N6CCC(C(O)=O)CC6
Relative Density.	1.33 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 6.76 mg/mL (10 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.48 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.4798 mL	7.3992 mL	14.7984 mL	73.9919 mL
5 mM	0.2960 mL	1.4798 mL	2.9597 mL	14.7984 mL
10 mM	0.1480 mL	0.7399 mL	1.4798 mL	7.3992 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc