Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Resomelagon (AP1189) 是具有口服活性的有效黑素皮质素受体 (MR) 激动剂,可诱导Ca2+流动和 ERK1/2 磷酸化。Resomelagon 显示出抗炎活性, 可用于研究肥胖和慢性炎症。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 1,270 | 5日内发货 | ||
5 mg | ¥ 2,350 | 5日内发货 | ||
25 mg | ¥ 8,160 | 6-8周 | ||
50 mg | ¥ 10,600 | 6-8周 | ||
100 mg | ¥ 16,400 | 6-8周 |
产品描述 | Resomelagon (AP1189) is a potent, orally active agonist of melanocortin receptor (MR) that induces Ca2+ mobilization and ERK1/2 phosphorylation. Resomelagon shows anti-inflammatory activity that can be used in obesity and chronic inflammation research [1] [2]. |
体外活性 | Resomelagon (AP1189) (0-1000 μM; 8 min; HEK293A cells) promotes melanocortin signal transduction through ERK1/2 phosphorylation and Ca 2+ mobilization [1]. Resomelagon (AP1189) (1 nM; 30 min; peritoneal macrophages) has anti-inflammatory activity and inhibits TNF-α release and efferocytosis [1]. Western Blot Analysis [1] Cell Line: HEK293A cells Concentration: 0-1000 μM Incubation Time: 8 minutes Result: Increased the expression of ERK1/2 phosphorylation in a dose-dependent manner. |
体内活性 | Resomelagon (AP1189) (0-10 mg/kg; i.p., i.v. and p.o.; for 24 h; male C57BL/6J wild-type (WT) and BALB/c mice) promotes resolution of acute inflammation in vivo [1]. Resomelagon (AP1189) (25-50 mg/kg; p.o.; daily, for 8 d; male C57BL/6J wild-type (WT) and BALB/c mice) reduces arthritis in mice [1]. Animal Model: Male C57BL/6J wild-type (WT) and BALB/c mice [1] Dosage: 0, 0.1, 1 and 10 mg/kg Administration: Oral administration, intraperitoneal injection and intravenous injection; for 24 hours Result: Inhibited neutrophil and monocyte infiltration in a dose-dependent manner. Animal Model: Male C57BL/6J wild-type (WT) and BALB/c mice [1] Dosage: 25 and 50 mg/kg Administration: Oral administration; daily; for 8 days Result: Reduced all signs of arthritis measured, including clinical score ( 42%), paw swelling ( 87%), proportion of animals with all four paws affected ( 50%), and the severity of the inflammation ( 70%). |
分子量 | 298.3 |
分子式 | C14H14N6O2 |
CAS No. | 1809420-71-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
Resomelagon 1809420-71-0 Inhibitor inhibitor inhibit