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

Alvelestat  (Synonyms: AZD9668)

製品番号: HY-15651 純度: 99.87%
COA 取扱説明書 Technical Support

Alvelestat (AZD9668) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM.

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Alvelestat

Alvelestat 構造式

CAS 番号 : 848141-11-7

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 92 在庫あり
Solution
10 mM * 1 mL in DMSO USD 92 在庫あり
Solid
1 mg $36 在庫あり
5 mg $77 在庫あり
10 mg $110 在庫あり
50 mg $330 在庫あり
100 mg $495 在庫あり
200 mg $750 在庫あり
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 11 publication(s) in Google Scholar

Other Forms of Alvelestat:

Alvelestat 関連抗体

Top Publications Citing Use of Products

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  • 純度とドキュメンテーション

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製品説明

Alvelestat (AZD9668) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM[1].

IC50 & Target

pIC: 7.9 nM; Ki: 9.4 nM; Kd: 9.5 nM (neutrophil elastas)[1]
体外実験

Alvelestat (20 μg/mL; 16 hours; HBE and A549 cells) treatment decreases cells death and decreases the levels of IL-1β, IL-6, and TNF-α in vitro[2].

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

Alvelestat 関連抗体

Cell Viability Assay[2]

Cell Line: Human bronchial epithelial cells (HBE) and human alveolar epithelial cells (A549)
Concentration: 20 μg/mL
Incubation Time: 16 hours
Result: Decreased cytotoxicity and inflammatory responses.
体内実験

Alvelestat (1-10 mg/kg; oral administration; twice daily; for 4 days; Female BALB/cJBomTac mice) treatment reduces the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1β[1].

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

Animal Model: Female BALB/cJBomTac mice exposed to smoke cigarette smoke[1]
Dosage: 1 mg/kg , 3 mg/kg , 6 mg/kg , 10 mg/kg
Administration: Oral administration; twice daily; for 4 days
Result: Reduced the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1β.
分子量

545.53

分子式

C25H22F3N5O4S
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC(C2=CC=NN2C)=C(C)N(C3=CC=CC(C(F)(F)F)=C3)C1=O)NCC4=NC=C(S(=O)(C)=O)C=C4
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 33 mg/mL (60.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8331 mL 9.1654 mL 18.3308 mL
5 mM 0.3666 mL 1.8331 mL 3.6662 mL
10 mM 0.1833 mL 0.9165 mL 1.8331 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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:  20% DMSO    60% PEG400    20% H2O

    Solubility: 25 mg/mL (45.83 mM); Suspended solution; Need ultrasonic

  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.87%

COA (249 KB) HNMR (178 KB) LCMS (97 KB)

取扱説明書 (2659 KB)
参考文献

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8331 mL 9.1654 mL 18.3308 mL 45.8270 mL
5 mM 0.3666 mL 1.8331 mL 3.6662 mL 9.1654 mL
10 mM 0.1833 mL 0.9165 mL 1.8331 mL 4.5827 mL
15 mM 0.1222 mL 0.6110 mL 1.2221 mL 3.0551 mL
20 mM 0.0917 mL 0.4583 mL 0.9165 mL 2.2913 mL
25 mM 0.0733 mL 0.3666 mL 0.7332 mL 1.8331 mL
30 mM 0.0611 mL 0.3055 mL 0.6110 mL 1.5276 mL
40 mM 0.0458 mL 0.2291 mL 0.4583 mL 1.1457 mL
50 mM 0.0367 mL 0.1833 mL 0.3666 mL 0.9165 mL
60 mM 0.0306 mL 0.1528 mL 0.3055 mL 0.7638 mL
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Alvelestat Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

Alvelestat848141-11-7AZD9668AZD 9668AZD-9668ElastaseInhibitorinhibitorinhibit

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Alvelestat
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