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BAY-85-8501

Catalog No. T12613L CAS 1161921-82-9

BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE; IC50 of 65 pM)

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BAY-85-8501, CAS 1161921-82-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 255.00
5 mg	In stock	$ 508.00
10 mg	In stock	$ 787.00
25 mg	In stock	$ 1,625.00
50 mg	In stock	$ 2,649.00
100 mg	In stock	$ 3,673.00
1 mL * 10 mM (in DMSO)	In stock	$ 518.00

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Purity: 98.63%

Biological Description

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Description	BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE; IC50 of 65 pM)
Targets&IC50	HNE:65 pM
In vivo	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. 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. BAY-85-8501 could inhibit MNE, the endogenous driver of inflammation and secondary injury, although with decreased potency. 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]. 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).

Molecular Weight	474.46
Formula	C22H17F3N4O3S
CAS No.	1161921-82-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 200 mg/mL (421.53 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BAY-85-8501 1161921-82-9 Proteases/Proteasome Serine Protease inhibit Elastase Inhibitor BAY 85 8501 BAY858501 inhibitor

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