1. Metabolic Enzyme/Protease
  2. Elastase
  3. AE-3763

AE-3763 

Cat. No.: HY-19406
Handling Instructions

AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC50 of 29 nM.

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

AE-3763 Chemical Structure

AE-3763 Chemical Structure

CAS No. : 291778-77-3

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5 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC50 of 29 nM.

IC50 & Target

IC50: 29 nM (Human neutrophil elastase)[1]

In Vitro

AE-3763 exhibits potent in vitro inhibitory activity against human neutrophil elastase as well as extremely high solubility and stability in water[1].

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

In Vivo

Edema and leukocytes infiltration into the lung are significantly inhibited by infusion of AE-3763. AE3763 significantly improves survival rate by 24 h in a mouse model of fatal shock associated with multiple organ dysfunction. AE-3763 dose-dependently prevents hemorrhage when given intravenously by infusion (ED50: 0.42 mg/kg/h) or by bolus injection (1.2 mg/kg). With regard to the toxicity of AE-3763 in mice, the results of a preliminary study have shown no overt toxic effect even at the high dose of 300 mg/kg, iv[1].

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

Molecular Weight

549.54

Formula

C₂₃H₃₄F₃N₅O₇

CAS No.

291778-77-3

SMILES

O=C(O)CN1CCN(CC(N[[email protected]](C(N2[[email protected]](C(N[[email protected]@H](C(C)C)C(C(F)(F)F)=O)=O)CCC2)=O)C(C)C)=O)C1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (30.33 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8197 mL 9.0985 mL 18.1970 mL
5 mM 0.3639 mL 1.8197 mL 3.6394 mL
10 mM 0.1820 mL 0.9099 mL 1.8197 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 1.67 mg/mL (3.04 mM); Clear solution

  • 2.

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

    Solubility: ≥ 1.67 mg/mL (3.04 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (3.04 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice[1]

D-Galactosamine shock is induced in C3H/HeN mice (6-7 w, 22-25 g). AE-3763 (10 or 100 mg/kg) is administrated intraperitoneally six times at 2 h interval. Control animals receive the vehicle (PBS) instead of AE-3763. Animal’s survival rate is observed up to 24 h after shock induction[1].

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

References
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Keywords:

AE-3763AE3763AE 3763ElastaseInhibitorinhibitorinhibit

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Product Name:
AE-3763
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HY-19406
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