2. Metabolic Enzyme/Protease
  3. Elastase
  4. FK706

FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect.

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FK706 Chemical Structure

FK706 Chemical Structure

CAS No. : 144055-55-0

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Based on 1 publication(s) in Google Scholar

FK706 Related Antibodies

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Description

FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect[1][2].

IC50 & Target

IC50: 83 nM (Human neutrophil elastase), 22 nM (Mouse neutrophil elastase) and 100 nM (Porcine pancreatic elastase)[1];
Ki: 4.2 nM (Human neutrophil elastase)[1]
In Vitro

FK706 effectively inhibits the hydrolysis of bovine neck ligament elastin (2 mg/mL final concentration) by human neutrophil elastase (4 μg/mL final concentration) with an IC50 value of 230 nM[1].
FK706 blocks the release of inflammatory chemokines, suppresses the expression of IL-8 and MCP-1 mRNA, and suppresses NF-κB activation. It seems possible that FK706 may directly blocks human lung fibroblasts activation of NF-κB, preventing expression of inflammatory chemokines during cigarette smoke–induced lung inflammation[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

FK706 Related Antibodies
In Vivo

FK706 (10-100 mg/kg; subcutaneous injection; for 1-6 hours; male C57BL mice) treatment significantly suppresses human neutrophil elastase (20 μg/paw)-induced paw edema in mice in a dose-dependent manner (47% inhibition at a dose of 100 mg/kg)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL mice (6 weeks old) injected with human neutrophil elastase[1]
Dosage: 10 mg/kg, 32 mg/kg, 100 mg/kg
Administration: Subcutaneous injection; for 1 hour, 2 hours, 4 hours, 6 hours
Result: Significantly suppressed human neutrophil elastase-induced paw edema in mice in a dose-dependent manner.
Molecular Weight

592.54

Formula

C26H32F3N4NaO7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC(C(C)C)C(C(F)(F)F)=O)[C@H]1N(C([C@H](C(C)C)NC(C2=CC=C(C(NCC(O[Na])=O)=O)C=C2)=O)=O)CCC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 115 mg/mL (194.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 100 mg/mL (168.76 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6876 mL 8.4382 mL 16.8765 mL
5 mM 0.3375 mL 1.6876 mL 3.3753 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (8.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (8.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.6876 mL 8.4382 mL 16.8765 mL 42.1912 mL
5 mM 0.3375 mL 1.6876 mL 3.3753 mL 8.4382 mL
10 mM 0.1688 mL 0.8438 mL 1.6876 mL 4.2191 mL
15 mM 0.1125 mL 0.5625 mL 1.1251 mL 2.8127 mL
20 mM 0.0844 mL 0.4219 mL 0.8438 mL 2.1096 mL
25 mM 0.0675 mL 0.3375 mL 0.6751 mL 1.6876 mL
30 mM 0.0563 mL 0.2813 mL 0.5625 mL 1.4064 mL
40 mM 0.0422 mL 0.2110 mL 0.4219 mL 1.0548 mL
50 mM 0.0338 mL 0.1688 mL 0.3375 mL 0.8438 mL
60 mM 0.0281 mL 0.1406 mL 0.2813 mL 0.7032 mL
80 mM 0.0211 mL 0.1055 mL 0.2110 mL 0.5274 mL
100 mM 0.0169 mL 0.0844 mL 0.1688 mL 0.4219 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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FK706 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FK706144055-55-0FK 706FK-706ElastaseWater-solubleslow-bindingsynthetichumanserineproteasesporcineinflammatorydisordersInhibitorinhibitorinhibit

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