AZD7594 (Synonyms: AZD7594; AZ13189620) |
| رقم الكتالوجGC19051 |
AZD7594 هو مُعدِّل مستقبلات الجلوكوكورتيكويد الانتقائي غير الستيرويدي ، مع IC50 من 0.9 نانومتر.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1196509-60-0
Sample solution is provided at 25 µL, 10mM.
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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.
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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]. |
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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. |
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| Cas No. | 1196509-60-0 | SDF | |
| المرادفات | 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 | ||
| Formula | C32H32F2N4O6 | M.Wt | 606.62 |
| الذوبان | DMSO : ≥ 83.3 mg/mL (137.32 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6485 mL | 8.2424 mL | 16.4848 mL |
| 5 mM | 329.7 μL | 1.6485 mL | 3.297 mL |
| 10 mM | 164.8 μL | 824.2 μL | 1.6485 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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