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JNJ-10229570

Name: JNJ-10229570
Brand: TargetMol
SKU: T5464
Price: 112 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5464Cas No. 524923-88-4

Alias UNII-N9IX402L35, JNJ10229570, JNJ 10229570

JNJ-10229570 (UNII-N9IX402L35) is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids.

JNJ-10229570

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Purity: 98.41%

Catalog No. T5464Alias UNII-N9IX402L35, JNJ10229570, JNJ 10229570Cas No. 524923-88-4

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$112	In Stock	In Stock
5 mg	$198	In Stock	In Stock
10 mg	$313	In Stock	In Stock
25 mg	$496	In Stock	In Stock
50 mg	$689	In Stock	In Stock
100 mg	$892	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$226	In Stock	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:98.41%

Appearance:Solid

Color:Yellow

Resource Download

COA LCMS HNMR HPLC

Product Introduction

Bioactivity

Description	JNJ-10229570 (UNII-N9IX402L35) is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids.
Targets&IC50	MC5R (human):200 nM, MC1R (human):270 nM
In vitro	JNJ-10229570 demonstrates dose-dependent inhibition of sebaceous lipid production in cultured primary human sebocytes. Concurrently, JNJ-7818369 effectively prevents the attachment of 125I-NDP-α-MSH to cells featuring human MC1R and MC5R receptors, presenting IC50 values of 270±120 nM and 200±50 nM, respectively. Similar efficacy is observed with the compound's free base form. For both variations of the compound, the inhibitory action on MC4R is identical, with IC50 values reported at 240±170 nM. Notably, treatment with JNJ-10229570 at a concentration of 0.01 μM markedly suppresses lipid granule formation, achieving total inhibition at a concentration of 0.05 μM.
In vivo	Topical treatment with JNJ-10229570 on human skins transplanted onto SCID mice significantly reduced sebum-specific lipid production, sebaceous gland size, and the expression of the sebaceous differentiation marker epithelial-membrane antigen (EMA). Treatment with flutamide, a known inhibitor of sebum production, validates the human skin/SCID mouse experimental system for sebaceous secretion studies.
Cell Research	Radioligand binding assays were performed, with CHO-K1 cells over-expressing MC1R, and HEK-293 cells over-expressing MC4R or MC5R, using a single concentration of 125I-NDP-a-MSH and increasing concentrations of JNJ-7818369 or JNJ-10229570. IC50 values for inhibition of radioligand binding were calculated by a non-linear, least squares regression method.
Animal Research	JNJ-10229570 (0.05%) and flutamide (5%) were dissolved in a vehicle of ethanol: propylene glycol (7:3).?20 ml/1.5 cm^2 were applied onto each skin xenograft, starting at three months posttransplantation.?Xenografts were treated once daily, 5 days/week, for 30 34 treatments.?Xenografts were then collected for histological examination and lipid analysis.?Each study was repeated with skin xenografts from at least 3 donors.?The vehicle had no effect on sebaceous glands differentiation or activity.
Synonyms	UNII-N9IX402L35, JNJ10229570, JNJ 10229570

Chemical Properties

Molecular Weight	389.47
Formula	C₂₂H₁₉N₃O₂S
Cas No.	524923-88-4
Smiles	COc1ccccc1-c1n\c(=N\c2ccccc2)sn1-c1ccccc1OC
Relative Density.	1.22 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: 62.5 mg/mL (160.47 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.14 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	2.5676 mL	12.8380 mL	25.6759 mL	128.3796 mL
5 mM	0.5135 mL	2.5676 mL	5.1352 mL	25.6759 mL
10 mM	0.2568 mL	1.2838 mL	2.5676 mL	12.8380 mL
20 mM	0.1284 mL	0.6419 mL	1.2838 mL	6.4190 mL
50 mM	0.0514 mL	0.2568 mL	0.5135 mL	2.5676 mL
100 mM	0.0257 mL	0.1284 mL	0.2568 mL	1.2838 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