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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 |
|---|
| CRN04894
CRN04894 is an orally active MC2R antagonist that demonstrates in vivo efficacy in rat model of adrenocorticotropic hormone (ACTH)-stimulated corticosterone secretion. |
| BMS-470539
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. |
| PF-00446687
PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. |
| BMS-470539 dihydrochloride
BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. |
| Undecylenoyl phenylalanine
Undecylenoyl phenylalanine is an antagonist for α-melanocyte-stimulating hormone (MSH) and β-adrenergic receptor (β-ADR) to reduce the melanogenesis in melanocytes. |
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