BAY-85-8501 - 10mM in DMSO , CAS No.1161921-82-9

CAS: 1161921-82-9 Cat. No.: B656657 Formula: C₂₂H₁₇F₃N₄O₃S Peso molecolare: 474.46 PubChem CID: 66601502

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE) , with an IC 50 of 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. 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 (K i =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 (K i =6 nM) in this second setup . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:IC50: 65 pM (HNE)

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE) , with an IC 50 of 65 pM.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

INHIBITOR

Nomi e identificatori

• Isomeri SMILES: CC1=C([C@H](N(C(=O)N1C2=CC=CC(=C2)C(F)(F)F)C)C3=C(C=C(C=C3)C#N)S(=O)(=O)C)C#N
• CAS alternativo: 1161921-82-9
• PubChem CID: 66601502
• Termini MeSH: 4-(4-cyano-2-(methylsulfonyl)phenyl)-3,6-dimethyl-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2,3,4-tetrahydropyrimidine-5-carbonitrile;BAY 85-8501
• Peso molecolare: 474.46

Obiettivi associati (umani)

ELANE Tclin Neutrophil elastase (4 Activities)

Discover Target: ELANE

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1161921-82-9, the molecular formula is C22H17F3N4O3S, and the molecular weight is 474.46 g/mol.