| Name | JNJ-10229570 |
| 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. |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 25 mg/mL (64.19 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.14 mM), Sonication is recommended.
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| Keywords | MelanocortinReceptor | melanocortin-5 receptor (MC5R) | melanocortin-1 receptor | Melanocortin Receptor | MC Receptor | JNJ-10229570 | Inhibitor | inhibit |
| Inhibitors Related | (±)-Eriodictyol | α-MSH | 4-Methyl-6-Methoxycoumarin | Fenoprofen Calcium | α-MSH acetate | BMS-470539 dihydrochloride | Bremelanotide | ACTH (1-17) acetate | Tetracosactide acetate | 2-MNG | Undecylenoyl phenylalanine | Bremelanotide Acetate |
| Related Compound Libraries | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Anti-Obesity Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library |
United States
