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JNJ-10229570

Cat. No. M10515

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JNJ-10229570 Structure
Synonym:

UNII-N9IX402L35; JNJ10229570

Size Price Availability Quantity
10mM*1mL in DMSO USD 290 In stock
1mg USD 100 In stock
5mg USD 270 In stock
10mg USD 430 In stock
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Quality Control & Documentation
Biological Activity

JNJ-10229570 (UNII-N9IX402L35) is is a novel melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R) antagonist, which inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R with IC50 values of 270 nM and 200 nM, respectively. JNJ-10229570 dose dependently inhibits the production of sebaceous lipids in cultured primary human sebocytes.

In vivo, topical treatment with JNJ-10229570 of human skins transplanted onto SCID mice result in a marked decrease in sebum-specific lipid production, sebaceous gland's size and the expression of the sebaceous differentiation marker epithelial-membrane antigen (EMA). Topical treatment with 0.05% JNJ-10229570 leads to a distinct reduction in both the steady-state and the newly-synthesized sebum-specific lipids, with lesser effects on triglycerides and cholesterol.

Protocol (for reference only)
Cell Experiment
Cell lines differentiated sebocytes
Preparation method Nile red assay. Briefly, differentiated sebocytes grown in 96-well plates were treated with or without 1 uM of JNJ-10229570 (8 repeats, 8 days), washed once, incubated in 1 uM Nile red and 0.001% Pluronic F127 (4 h, RT, dark), and washed again. Fluorescence (485 nm excitation, 565 nm emission) was determined in a SPECTRAmax Gemini-EM plate reader (Molecular Devices, Sunnyvale, CA) by SoftMax Pro program.
Concentrations 1 uM
Incubation time -
Animal Experiment
Animal models Human skins transplanted onto SCID mice
Formulation dissolved in a vehicle of ethanol: propylene glycol (7:3)
Dosages JNJ-10229570 (0.05%) 20 ml/1.5 cm2
Administration applied onto each skin xenograft once daily, 5 days/week, for 30-34 treatments
Chemical Information
Molecular Weight 389.47
Formula C22H19N3O2S
CAS Number 524923-88-4
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Magdalena Eisinger, et al. J Dermatol Sci. A melanocortin receptor 1 and 5 antagonist inhibits sebaceous gland differentiation and the production of sebum-specific lipids

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Keywords: JNJ-10229570, UNII-N9IX402L35; JNJ10229570 supplier, Melanocortin Receptor, inhibitors, activators

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