store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PD 168368 是一种新型有效且具有竞争性和选择性的非肽类神经调节蛋白 B 受体 (NMB-R) 拮抗剂,对胃泌素释放肽受体 (GRPR)具有抑制作用。PD 168368 是一种高效的 FPR1/FPR2/FPR3 的混合激动剂。
产品描述 | PD 168368 is a novel, potent, competitive and selective nonpeptide neuromodulin B receptor (NMB-R) antagonist with inhibitory effects on the gastrin-releasing peptide receptor (GRPR).PD 168368 is a potent mixed agonist of FPR1/FPR2/FPR3. |
体外活性 |
PD 168368 exhibits high activity and induces [Ca2+]I release in human neutrophils, with EC50 values in the nanomolar range[3]. In the human breast cancer cell line MDA-MB-231, PD 168368 suppresses migration and invasion. It also reduces epithelial-mesenchymal transition (EMT) by upregulating E-cadherin and downregulating vimentin. At a concentration of 5 μM, PD 168368 inhibits migration and invasiveness in breast cancer cells[4]. Furthermore, at a concentration of 10 μM, PD 168368 suppresses the activation of the mTOR/p70S6K/4EBP1 and AKT/GSK-3β pathways in breast cancer cells[4]. |
体内活性 | In mice, PD 168368 potently inhibits the in vivo metastasis of breast cancer. Administered at a dose of 1.2 mg/kg through intraperitoneal injection for 30 days, PD 168368 effectively inhibits breast cancer metastasis[4]. |
别名 | PD168368 |
分子量 | 554.64 |
分子式 | C31H34N6O4 |
CAS No. | 204066-82-0 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20 mg/mL(36.06 mM), Sonication is recommended.
DMF: 5 mg/mL(9.01 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / DMF | 1 mM | 1.803 mL | 9.0149 mL | 18.0297 mL | 45.0743 mL |
5 mM | 0.3606 mL | 1.803 mL | 3.6059 mL | 9.0149 mL | |
DMSO | 10 mM | 0.1803 mL | 0.9015 mL | 1.803 mL | 4.5074 mL |
20 mM | 0.0901 mL | 0.4507 mL | 0.9015 mL | 2.2537 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。
PD 168368 204066-82-0 GPCR/G Protein Bombesin Receptor PD-168368 PD168368 Inhibitor inhibitor inhibit