Powder: -20°C for 3 years
In solvent: -80°C for 2 years
BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE; IC50 of 65 pM)
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 200 mg/mL (421.53 mM), Need ultrasonic
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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BAY-85-8501 1161921-82-9 Proteases/Proteasome Serine Protease inhibit Elastase Inhibitor BAY 85 8501 BAY858501 inhibitor