| 名称 | JNJ-10229570 |
| 描述 | 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. |
| 细胞实验 | 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. |
| 动物实验 | 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. |
| 体外活性 | 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. |
| 体内活性 | 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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 62.5 mg/mL (160.47 mM)
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| 关键字 | MC Receptor | Inhibitor | JNJ-10229570 | inhibit | Melanocortin Receptor |
| 相关产品 | HS 014 acetate(207678-81-7 free base) | MCL0020 | Beta-MSH (1-22) (human) acetate | ACTH (1-17) acetate | Neuropeptide EI, rat acetate | [D-Trp8]-γ-MSH acetate(321351-81-9 free base) | a-MSH, amide Acetate(581-05-5 free base) | Undecylenoyl phenylalanine | ACTH 11-24 acetate(4237-93-8 free base) | Melanotan (MT)-II | HS024 | Nonapeptide-1 acetate salt (158563-45-2 free base) |
| 相关库 | 经典已知活性库 | 神经信号分子库 | 膜蛋白靶向化合物库 | 抗肥胖化合物库 | 抑制剂库 | NO PAINS 化合物库 | 已知活性化合物库 | GPCR靶点分子库 |
United States
