BAY-85-8501 |
| رقم الكتالوجGC31564 |
BAY-85-8501 هو مثبط انتقائي وقابل للانعكاس وقوي لمانع الإيلاستاز البشري (HNE) ، مع IC50 من 65 pM
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1161921-82-9
Sample solution is provided at 25 µL, 10mM.
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BAY-85-8501 is a selective and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM.
In this model the exogenous HNE noxa is the primary cause of injury and lung hemorrhage. Based on picomolar potency against HNE as well as single digit potency versus MNE, BAY-85-8501 (29) completely prevents the development of lung injury and subsequent inflammation when administered 1 h prior to the HNE noxa. In the 0.01 mg/kg dose group, hemoglobin concentration is already significantly decreased. At a dose of 0.1 mg/kg, a significant effect on neutrophil count is observed. In this setup, efficacy is predominantly driven by potency against HNE (Ki=0.08 nM). As the highly HNE-selective inhibitor BAY 85-8501 has no effect on PPE, BAY-85-8501 could not prevent the primary lung injury in this setup. Nevertheless, BAY-85-8501 could inhibit MNE, the endogenous driver of inflammation and secondary injury, although with decreased potency. Consequently, the effects of BAY-85-8501 on inflammation and secondary injury are weaker at this point, and only observed at 30-fold higher doses. Efficacy is predominantly driven by potency against MNE (Ki=6 nM) in this second setup[1].
[1]. Von Nussbaum F, et al. Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem. 2015 Jul;10(7):1163-73.
Animal experiment: | Mice[1]Elastaseinduced lung failure in mice, rats or hamsters is a widely used animal model of acute lung failure. The animals are treated 1 hour prior to orotracheal instillation of human neutrophil elastase (HNE) or porcine pancreatic elastase (PPE). In this study, each mouse receives BAY-85-8501 with different concentrations (0.003, 0.01, 0.03, 0.1, 0.3, 3, 10, 30 mg/kg) by P.O.[1]. |
References: [1]. Von Nussbaum F, et al. Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem. 2015 Jul;10(7):1163-73. | |
| Cas No. | 1161921-82-9 | SDF | |
| Canonical SMILES | N#CC1=C(C)N(C2=CC=CC(C(F)(F)F)=C2)C(N(C)[C@@H]1C3=CC=C(C#N)C=C3S(=O)(C)=O)=O | ||
| Formula | C22H17F3N4O3S | M.Wt | 474.46 |
| الذوبان | Soluble in DMSO | 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 | 2.1077 mL | 10.5383 mL | 21.0766 mL |
| 5 mM | 0.4215 mL | 2.1077 mL | 4.2153 mL |
| 10 mM | 0.2108 mL | 1.0538 mL | 2.1077 mL |
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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
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- Purity: >99.50%
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