Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JNJ-10229570 (UNII-N9IX402L35) 是肾上腺皮质受体 1 和肾上腺皮质受体 5 的拮抗剂,可抑制皮脂腺分化和皮质特异性脂质的产生,其抑制125I-NDP-α-MSH 和人类细胞中 MC1R 和 MC5R 结合的IC50值分别为 270 nM 和 200 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 917 | 现货 | ||
5 mg | ¥ 2,390 | 现货 | ||
10 mg | ¥ 3,730 | 现货 | ||
25 mg | ¥ 5,970 | 现货 | ||
50 mg | ¥ 8,420 | 现货 | ||
100 mg | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,650 | 现货 |
产品描述 | 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. |
靶点活性 | MC5R (human):200 nM, MC1R (human):270 nM |
体外活性 | JNJ-10229570 dose dependently inhibits the production of sebaceous lipids in cultured primary human sebocytes. JNJ-7818369 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50s of 270±120 and 200±50 nM, respectively. Nearly-identical results are obtained with the free base form of the compound. Binding to MC4R of both forms of the compound is equipotent, with IC50s of 240±170 nM. JNJ-10229570-treated cells show strong inhibition of lipid granules at 0.01 μM, and complete inhibition at 0.05 μM. |
体内活性 | Topical treatment with JNJ-10229570 of human skins transplanted onto SCID mice resulted 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).?Treatment with flutamide, a known inhibitor of sebum production, the human skin/SCID mouse experimental system for sebaceous secretion studies |
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. |
别名 | JNJ10229570, UNII-N9IX402L35, JNJ 10229570 |
分子量 | 389.47 |
分子式 | C22H19N3O2S |
CAS No. | 524923-88-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 62.5 mg/mL (160.47 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5676 mL | 12.838 mL | 25.6759 mL | 64.1898 mL |
5 mM | 0.5135 mL | 2.5676 mL | 5.1352 mL | 12.838 mL | |
10 mM | 0.2568 mL | 1.2838 mL | 2.5676 mL | 6.419 mL | |
20 mM | 0.1284 mL | 0.6419 mL | 1.2838 mL | 3.2095 mL | |
50 mM | 0.0514 mL | 0.2568 mL | 0.5135 mL | 1.2838 mL | |
100 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.6419 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
JNJ-10229570 524923-88-4 GPCR/G Protein Neuroscience Melanocortin Receptor MC Receptor Inhibitor inhibit JNJ10229570 UNII-N9IX402L35 JNJ 10229570 inhibitor