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Panadiplon

Panadiplon

产品编号 T28294   CAS 124423-84-3
别名: FG10571, FG-10571, FD-10571, PNU 78875, FG 10571, FD10571, FD 10571

Panadiplon (FG 10571) 是一种具有选择性的γ-氨基丁酸受体激动剂和5GABAA 的部分激动剂,是一种苯二氮卓类受体,可用于治疗焦虑症。Panadiplon 对 5GABAA 受体与 1GABAA 受体表现出选择性。

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Panadiplon Chemical Structure
Panadiplon, CAS 124423-84-3
规格 价格/CNY 货期 数量
1 mg ¥ 990 现货
5 mg ¥ 2,500 现货
10 mg ¥ 3,730 现货
25 mg ¥ 5,890 现货
50 mg ¥ 8,290 现货
100 mg ¥ 11,200 现货
千万补贴 助力科研
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产品目录号及名称: Panadiplon (T28294)
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纯度: 100%
纯度: 99.75%
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生物活性
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存储 & 溶解度
参考文献
产品描述 Panadiplon (FG 10571) is a selective gamma-aminobutyric acid receptor agonist and partial agonist of 5GABAA, a benzodiazepine receptor, used in the treatment of anxiety disorders.Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.
体外活性 Panadiplon (10 μg/ml; 48 h; under normoxic conditions; hepatocytes) reduced ATP and glycogen levels by 40% but did not cause an increase in LDH leakage. Cells treated with panadiplon, then exposed to hypoxia conditions, showed a significant level of injury compared to normoxic control cultures, and a further reduction in ATP. No additional decrease in glycogen was observed. In an attempt to prevent panadiplon-mediated injury, glycolytic substrates (dihydroxyacetone or pyruvate) were included during normoxic and hypoxic incubations. Both treatments reduced the level of LDH leakage produced by panadiplon during hypoxia. Cotreatment did not generally increase ATP or glycogen levels (compared to panadiplon treatment groups) during hypoxia, though individual experiments showed a slight increase in ATP levels. During normoxia, both cotreatments with panadiplon resulted in significantly higher glycogen levels than in panadiplon cultures alone. These results suggest that cellular glycogen and subsequently ATP levels are reduced during panadiplon exposure, metabolically predisposing hepatocytes to hypoxic injury.[2]
别名 FG10571, FG-10571, FD-10571, PNU 78875, FG 10571, FD10571, FD 10571
分子量 335.36
分子式 C18H17N5O2
CAS No. 124423-84-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (149.09 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9819 mL 14.9094 mL 29.8187 mL 74.5468 mL
5 mM 0.5964 mL 2.9819 mL 5.9637 mL 14.9094 mL
10 mM 0.2982 mL 1.4909 mL 2.9819 mL 7.4547 mL
20 mM 0.1491 mL 0.7455 mL 1.4909 mL 3.7273 mL
50 mM 0.0596 mL 0.2982 mL 0.5964 mL 1.4909 mL
100 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7455 mL

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TargetMol Library Books参考文献

1. Platt DM, et al. Contribution of alpha 1GABAA and alpha 5GABAA receptor subtypes to the discriminative stimulus effects of ethanol in squirrel monkeys. J Pharmacol Exp Ther. 2005;313(2):658-667. 2. Bacon JA, et al. Potentiation of hypoxic injury in cultured rabbit hepatocytes by the quinoxalinone anxiolytic, panadiplon. Toxicology. 1996;108(1-2):9-16. 3. Rowlett JK, et al. Discriminative stimulus effects of panadiplon (U-78875), a partial agonist at the benzodiazepine site, in pentobarbital-trained rhesus monkeys. Drug Alcohol Depend. 2001;61(3):229-236. 4. Ulrich RG, et al. Metabolic, idiosyncratic toxicity of drugs: overview of the hepatic toxicity induced by the anxiolytic, panadiplon. Chem Biol Interact. 2001;134(3):251-270. 5. Ulrich RG, et al. Disruption of mitochondrial activities in rabbit and human hepatocytes by a quinoxalinone anxiolytic and its carboxylic acid metabolite. Toxicology. 1998;131(1):33-47.
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相关化合物库

该产品包含在如下化合物库中:
膜蛋白靶向化合物库 神经退行性疾病化合物库 已知活性化合物库 经典已知活性库 神经递质受体化合物库

TargetMol Calculator剂量换算

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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。

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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。

Keywords

Panadiplon 124423-84-3 Membrane transporter/Ion channel Neuroscience GABA Receptor FG10571 PNU78875 FG-10571 PNU-78875 FD-10571 PNU 78875 FG 10571 FD10571 FD 10571 Inhibitor inhibitor inhibit

 

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