1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. JAK
  3. Londamocitinib

Londamocitinib  (Synonyms: AZD4604; JAK1-IN-7)

製品番号: HY-126294 純度: 99.79%
COA 取扱説明書 Technical Support

Londamocitinib (AZD4604) is a potent and selective JAK1 inhibitor with IC50 at 0.54 nM. Londamocitinib has anti-inflammatory activity.

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Londamocitinib

Londamocitinib 構造式

CAS 番号 : 2241039-81-4

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 739 在庫あり
Solution
10 mM * 1 mL in DMSO USD 739 在庫あり
Solid
1 mg $230 在庫あり
5 mg $560 在庫あり
10 mg $760 在庫あり
25 mg $1150 在庫あり
50 mg $1500 在庫あり
100 mg $2000 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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製品説明

Londamocitinib (AZD4604) is a potent and selective JAK1 inhibitor with IC50 at 0.54 nM. Londamocitinib has anti-inflammatory activity[1][2][3].

IC50 & Target[1]

JAK1

0.54 nM (IC50)

体外実験

Londamocitinib inhibits the phosphorylation of STAT6 in U937 cells induced by IL-4 or IL-13 (IC50 are 24 and 34 nM, respectively)[2].

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

体内実験

Londamocitinib (1 mg/kg, intravenous injection, single dose) can reduce the phosphorylation of STAT3 and STAT5 in the lung of obumin-induced asthmatic rats, inhibit pulmonary eosinophilia, and reduce advanced asthma response in the same model[3].

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

Animal Model: OVA-Induced Rat Model of Asthma[3]
Dosage: 1 mg/kg
Administration: i.v.
Result: Reduced the proportion of phosphorylated STAT3-positive cell nuclei.
臨床実験
分子量

599.65

分子式

C28H31F2N7O4S

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

FC1=C(S(C)(=O)=O)C=CC=C1NC2=NC(C3=CNC4=C3C=CC=C4NC([C@@H](COC)N5CCN(C)CC5)=O)=C(F)C=N2

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 : 71.43 mg/mL (119.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6676 mL 8.3382 mL 16.6764 mL
5 mM 0.3335 mL 1.6676 mL 3.3353 mL
10 mM 0.1668 mL 0.8338 mL 1.6676 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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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

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C2

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体積 (終了)

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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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.17 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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, 6 months; -20°C, 1 month. 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
DMSO 1 mM 1.6676 mL 8.3382 mL 16.6764 mL 41.6910 mL
5 mM 0.3335 mL 1.6676 mL 3.3353 mL 8.3382 mL
10 mM 0.1668 mL 0.8338 mL 1.6676 mL 4.1691 mL
15 mM 0.1112 mL 0.5559 mL 1.1118 mL 2.7794 mL
20 mM 0.0834 mL 0.4169 mL 0.8338 mL 2.0845 mL
25 mM 0.0667 mL 0.3335 mL 0.6671 mL 1.6676 mL
30 mM 0.0556 mL 0.2779 mL 0.5559 mL 1.3897 mL
40 mM 0.0417 mL 0.2085 mL 0.4169 mL 1.0423 mL
50 mM 0.0334 mL 0.1668 mL 0.3335 mL 0.8338 mL
60 mM 0.0278 mL 0.1390 mL 0.2779 mL 0.6948 mL
80 mM 0.0208 mL 0.1042 mL 0.2085 mL 0.5211 mL
100 mM 0.0167 mL 0.0834 mL 0.1668 mL 0.4169 mL
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  • 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.

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製品名:
Londamocitinib
製品番号:
HY-126294
数量:
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