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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.
| 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 |
| 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 |
| Related Melanocortin Receptor Products |
|---|
| α-MSH
α-MSH (α-Melanocyte-stimulating hormone) is a tridecapeptide, mostly produced by the cells in the brain, pituitary and circulation. |
| Melanotan I acetate
Melanotan I acetate is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH). *This compound is unstable in solutions, freshly prepared is recommended. |
| Setmelanotide
Setmelanotide is a selective agonist of the MC4 receptor, with EC50 values of 0.27 nM and 0.28 nM for human and rat MC4R, respectively. |
| Bremelanotide Acetate
Bremelanotide Acetate (PT-141 Acetate) is a peptide containing seven amino acids and is also a macrocyclic compound. In addition, Bremelanotide Acetate is an agonist of the melanocortin 4 receptor (MC4R). |
| β-Melanocyte Stimulating Hormone TFA, human
β-Melanocyte Stimulating Hormone TFA, human is a 22-residue peptide, which acts as an endogenous melanocortin-4 receptor (MC4-R) agonist. |
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