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CDPPB

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纯度: 99.16%

货号 T22641Cas号 781652-57-1

CDPPB 是选择性和脑渗透性的代谢型谷氨酸受体亚型5 (mGluR5) 阳性变构的调节剂,在表达人类 mGluR5 的中国仓鼠卵巢细胞中的 EC50值为 27 nM。它为开发抗精神病药提供了一种可能性。

CDPPB
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CDPPB

一键复制产品信息
Rating icon 很棒

纯度: 99.16%

货号 T22641Cas号 781652-57-1

CDPPB 是选择性和脑渗透性的代谢型谷氨酸受体亚型5 (mGluR5) 阳性变构的调节剂,在表达人类 mGluR5 的中国仓鼠卵巢细胞中的 EC50值为 27 nM。它为开发抗精神病药提供了一种可能性。

规格价格库存数量
1 mg
¥ 365
现货
5 mg
¥ 828
现货
10 mg
¥ 1,320
现货
25 mg
¥ 2,430
现货
50 mg
¥ 3,980
现货
100 mg
¥ 5,530
现货
200 mg
¥ 7,570
现货
1 mL x 10 mM (in DMSO)
¥ 663
现货
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产品介绍


CDPPB AI Summary
CDPPB has been shown to potentiate the activity of human and rat metabotropic glutamate receptor 5 (mGluR5), demonstrating a fold potentiation of 4.0 in CHO cells overexpressing human mGluR5 and 4.3 towards rat mGluR5. It exhibits EC50 values of 10.0 nM for human mGluR5 and 20.0 nM for rat mGluR5 in transfected CHO cells. Additionally, its Ki value for human mGluR5 is 250.0 nM in a displacement assay. The compound shows positive allosteric modulation in calcium mobilization assays with EC50 values of 177.83 nM and 98.0 nM for human and rat mGluR5, respectively, in HEK293 cells. CDPPB demonstrates a LogD7.4 value of 3.82, suggesting favorable lipophilicity and membrane permeability. Moreover, CDPPB exhibits antiviral activity by inhibiting SARS-CoV-2-induced cytotoxicity in Caco-2 and VERO-6 cells at a 10 µM concentration, with inhibition rates of 0.24% and 0.53%, respectively. It also exhibits an inhibitory effect on the SARS-CoV-2 3CL-Pro protease, with an inhibition percentage of 5.339%. Inhibition of human HDAC6 was observed with percentages of 69.99% and 12.17% using different peptide substrates. Thermally, CDPPB affects various protein domain stabilities, increasing stability of domains such as S229-K512 and M626-G746, while decreasing stability of others like N44-E168 and M1-K294. Furthermore, the compound shows a range of effects on GPCR targets in beta-arrestin recruitment assays, inhibiting targets like FPR2 and ADRB2, while activating receptors such as C5AR1 and S1PR1. These diverse bioactivities suggest it may modulate multiple physiological processes regulated by these receptors..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5).
靶点活性
mGluR5:27 nM (EC50)
化学信息
分子量364.4
分子式C23H16N4O
CAS No.781652-57-1
SmilesO=C(Nc1cc(nn1-c1ccccc1)-c1ccccc1)c1cccc(c1)C#N
密度1.203g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 3.65 mg/mL (10.02 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.7442 mL13.7212 mL27.4424 mL137.2119 mL
5 mM0.5488 mL2.7442 mL5.4885 mL27.4424 mL
10 mM0.2744 mL1.3721 mL2.7442 mL13.7212 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

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:
TargetMol | Animal experiments 比如您的给药剂量是10 mg/kg,每只动物体重20g,给药体积100 μLTargetMol | Animal experiments 一共给药动物10只,您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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