1. Metabolic Enzyme/Protease
  2. Elastase
  3. BAY-678

BAY-678 

Cat. No.: HY-111457A Purity: 98.16% ee.: 99.38%
Handling Instructions

BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

For research use only. We do not sell to patients.

BAY-678 Chemical Structure

BAY-678 Chemical Structure

CAS No. : 675103-36-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 260 In-stock
Estimated Time of Arrival: December 31
50 mg USD 460 In-stock
Estimated Time of Arrival: December 31
100 mg USD 790 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

IC50 & Target

IC50: 20 nM (HNE)[1].

In Vitro

BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. The Ki value of BAY-678 for MNE is 700 nM. BAY-678 is the 4th generation inhibitor of HNE[1]. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC)[2]. BAY-678 has more than 2,000-fold selectivity in a panel of 21 serine proteases[3].

In Vivo

BAY-678 (17) reveals significant efficacy in preclinical models of ALI and lung emphysema, demonstrating their anti-inflammatory and anti-remodeling mode of action. Additionally, BAY-678 (17) has shown significant beneficial pulmonary hemodynamic and vascular effects in models of PAH in rats and mice[2].

Molecular Weight

400.35

Formula

C₂₀H₁₅F₃N₄O₂

CAS No.

675103-36-3

SMILES

N#CC1=NC=C([[email protected]](C(C(C)=O)=C(C)N2C3=CC=CC(C(F)(F)F)=C3)NC2=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (249.78 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4978 mL 12.4891 mL 24.9781 mL
5 mM 0.4996 mL 2.4978 mL 4.9956 mL
10 mM 0.2498 mL 1.2489 mL 2.4978 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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BAY-678
Cat. No.:
HY-111457A
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