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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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|---|
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Adrenocorticotropic Hormone (ACTH) (4-10), human is a melanocortin 4 (MC4R) receptor agonist. |
| γ1-MSH
γ1-MSH is a melanocortin MC3 receptor agonist, with a Ki of 34 nM for the rat MC3 receptor. |
| γ-1-Melanocyte Stimulating Hormone (MSH), amide
γ-1-Melanocyte Stimulating Hormone (MSH), amide is a 11-amino acid peptide. |
| JKC363
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| ACTH (11-24)
ACTH (11-24) is an adrenocorticotropic hormone (ACTH) receptor antagonist. |
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