Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JNJ-63533054 是一种选择性的,具有口服活性的GPR139激动剂,对人GPR139的EC50为 16 nM。它可穿过血脑屏障,对 GPR139 的选择性高于其他 GPCR、离子通道和转运蛋白。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 235 | 现货 | ||
5 mg | ¥ 525 | 现货 | ||
10 mg | ¥ 898 | 现货 | ||
25 mg | ¥ 1,620 | 现货 | ||
50 mg | ¥ 2,420 | 现货 | ||
100 mg | ¥ 3,580 | 现货 | ||
500 mg | ¥ 7,750 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 525 | 现货 |
产品描述 | JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM. |
靶点活性 | GPR139:16 Nm(EC50) |
体外活性 | JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays. JNJ-63533054 is found to be clean of any cross reactivity as judged by an external selectivity panel of 50 known GPCRs, ion channels, and transporters as well as our own internal whole cell lead generation biology selectivity panel. |
体内活性 | JNJ-63533054 is found to cross the blood-brain barrier and have good drug-like properties amenable for oral dosing in rat. JNJ-63533054 exhibits good stability in both human and rat microsomes and high solubility in aqueous media, and no DDI potential was found. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 = 63 ± 24 nM, mouse EC50 = 28 ± 7 nM). |
别名 | JNJ 63533054 |
分子量 | 316.78 |
分子式 | C17H17ClN2O2 |
CAS No. | 1802326-66-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 31.7 mg/mL(100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1568 mL | 15.7838 mL | 31.5676 mL | 78.9191 mL |
5 mM | 0.6314 mL | 3.1568 mL | 6.3135 mL | 15.7838 mL | |
10 mM | 0.3157 mL | 1.5784 mL | 3.1568 mL | 7.8919 mL | |
20 mM | 0.1578 mL | 0.7892 mL | 1.5784 mL | 3.946 mL | |
50 mM | 0.0631 mL | 0.3157 mL | 0.6314 mL | 1.5784 mL | |
100 mM | 0.0316 mL | 0.1578 mL | 0.3157 mL | 0.7892 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-63533054 1802326-66-4 Endocrinology/Hormones GPCR/G Protein GPR L-tryptophan blood-brain oral CNS L-phenylalanine G Protein-Coupled Receptor 139 barrier JNJ 63533054 Inhibitor GPR139 inhibit JNJ63533054 inhibitor