BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophilelastase(HNE), with anIC₅₀of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

IC50: 20 nM (HNE)^[1].

BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC₅₀of 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].

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].

400.35

Solid

C₂₀H₁₅F₃N₄O₂

675103-36-3

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL(249.78 mM)

Ethanol : ≥ 4.76 mg/mL(11.89 mM)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.24 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.24 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。