AZD7594
(Synonyms: AZD7594; AZ13189620) 目录号 : GC19051AZD7594 是一种有效的选择性非甾体糖皮质激素受体调节剂,IC50 为 0.9 nM。
Cas No.:1196509-60-0
Sample solution is provided at 25 µL, 10mM.
AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC50 of 0.9 nM.
AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC50 of 0.9 nM. AZD7594 shows no effect on progesterone receptor, mineralocorticoid receptor, Androgen receptor, ERα or ERβ (IC50, > 10 uM).
AZD7594 has anti-inflammatory activity, and efficiently inhibits rat lung edema[1].
References:
[1]. Hemmerling M, et al. Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases. J Med Chem. 2017 Oct 26;60(20):8591-8605.
Kinase experiment: | Androgen receptor (AR) binding is measured in a fluorescence polarization ligand displacement assay using commercially available reagents, including recombinant rat AR ligand binding domain tagged with His and GST, Fluormone labelled AL Green ligand, DTT and AR Green assay buffer (containing protein stabilizing agents and glycerol, pH 7.5). Test compounds (AZD7594, etc.) and controls in 100% DMSO are added to 384-well plates in 0.2 μL. AR-LBD and Fluomone AL Green in AR Green assay buffer are added to 12.5 nM and 0.5 nM in a final volume of 15 μL. Plates are incubated in the dark at room temperature for 4-6 hours before fluorescence polarization is measured (excitation 485 nm, emission 530 nm). The shift in polarization value in the presence of test compounds (AZD7594, etc.) is used to determine relative affinity of test compounds for AR. The minimum and maximum values are determined in the in the presence of testosterone (1.3 μM) and in the absence of test compound. The molar concentration of compound producing 50% binding (IC50) of AR is mesured[1]. |
References: [1]. Hemmerling M, et al. Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases. J Med Chem. 2017 Oct 26;60(20):8591-8605. |
Cas No. | 1196509-60-0 | SDF | |
别名 | AZD7594; AZ13189620 | ||
Canonical SMILES | O=C(N[C@H]1COCC1)C2=CC=CC(N3N=CC4=C3C=CC(O[C@H](C5=CC=C(OCCO6)C6=C5)[C@@H](NC(C(F)(F)C)=O)C)=C4)=C2 | ||
分子式 | C32H32F2N4O6 | 分子量 | 606.62 |
溶解度 | DMSO : ≥ 83.3 mg/mL (137.32 mM) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.6485 mL | 8.2424 mL | 16.4848 mL |
5 mM | 0.3297 mL | 1.6485 mL | 3.297 mL |
10 mM | 0.1648 mL | 0.8242 mL | 1.6485 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
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