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BAY-85-8501

Name: BAY-85-8501
Brand: TargetMol
SKU: T12613L
Price: 88 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12613LCas No. 1161921-82-9

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

BAY-85-8501

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Purity: 99.16%

Catalog No. T12613LCas No. 1161921-82-9

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

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$88	In Stock	In Stock
2 mg	$130	In Stock	In Stock
5 mg	$223	In Stock	In Stock
10 mg	$331	In Stock	In Stock
25 mg	$595	In Stock	In Stock
50 mg	$834	In Stock	In Stock
100 mg	$1,150	-	In Stock
1 mL x 10 mM (in DMSO)	$232	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.16%

Appearance:Solid

Color:White

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COA LCMS HPLC HNMR

Product Introduction

Bioactivity

Description	BAY-85-8501 is a selective, reversible, and potent inhibitor of Human Neutrophil Elastase (HNE) with an IC50 of 65 pM.
Targets&IC50	HNE:65 pM
In vivo	In this study, the exogenous compound HNE noxa is identified as the primary cause of lung injury and hemorrhage. BAY-85-8501 (29), due to its picomolar potency against HNE and high effectiveness against MNE, completely prevents lung injury and subsequent inflammation if administered one hour before exposure to HNE noxa. Despite its high selectivity for HNE inhibition, BAY-85-8501 does not prevent primary lung injury caused by PPE since it has no effect on it. However, BAY-85-8501 can inhibit MNE, an endogenous promoter of inflammation and secondary lung injury, albeit with lower potency. The prevention of inflammation and secondary injury by BAY-85-8501 is less pronounced and requires doses 30 times higher than standard. Its effectiveness primarily relies on its ability to inhibit MNE (Ki=6 nM) in these cases. At a dosage of 0.01 mg/kg, a significant reduction in hemoglobin concentration is noted, and at 0.1 mg/kg, a notable decrease in neutrophil count is observed, indicating efficacy is largely dependent on its potency against HNE (Ki=0.08 nM) in this scenario.

Chemical Properties

Molecular Weight	474.46
Formula	C₂₂H₁₇F₃N₄O₃S
Cas No.	1161921-82-9
Smiles	CN1[C@@H](C(C#N)=C(C)N(C1=O)c1cccc(c1)C(F)(F)F)c1ccc(cc1S(C)(=O)=O)C#N
Relative Density.	1.49 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 200 mg/mL (421.53 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.54 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1077 mL	10.5383 mL	21.0766 mL	105.3830 mL
5 mM	0.4215 mL	2.1077 mL	4.2153 mL	21.0766 mL
10 mM	0.2108 mL	1.0538 mL	2.1077 mL	10.5383 mL
20 mM	0.1054 mL	0.5269 mL	1.0538 mL	5.2691 mL
50 mM	0.0422 mL	0.2108 mL	0.4215 mL	2.1077 mL
100 mM	0.0211 mL	0.1054 mL	0.2108 mL	1.0538 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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