2. Metabolic Enzyme/Protease Neuronal Signaling Immunology/Inflammation GPCR/G Protein Anti-infection
  3. Endogenous Metabolite Histamine Receptor SARS-CoV Influenza Virus
  4. Ketotifen

Ketotifen  (Synonyms: HC 20-511)

製品番号: HY-B0157 純度: 99.94%
COA 取扱説明書 Technical Support

Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Ketotifen

Ketotifen 構造式

CAS 番号 : 34580-13-7

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 38 在庫あり
Solution
10 mM * 1 mL in DMSO USD 38 在庫あり
Solid
25 mg $35 在庫あり
50 mg $53 在庫あり
100 mg $85 在庫あり
200 mg   お問い合わせ  
500 mg   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

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Other Forms of Ketotifen:

Ketotifen 関連抗体

Top Publications Citing Use of Products

Endogenous Metabolite アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Human Endogenous Metabolite Microbial Metabolite

Histamine Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention[1][2][3][4].

IC50 & Target

H1 Receptor

 

Cellular Effect
Cell Line Type Value Description References
CHO-K1 IC50
1 nM
Compound: Ketotifen
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
[PMID: 21470866]
RBL-2H3 IC50
27.9 μM
Compound: Ketotifen
Antiallergic activity in rat RBL-2H3 cell model assessed as inhibition rate of IgE-mediated degranulation in by measuring beta-aminosidase
Antiallergic activity in rat RBL-2H3 cell model assessed as inhibition rate of IgE-mediated degranulation in by measuring beta-aminosidase
[PMID: 38640354]
RBL-2H3 IC50
35.2 μM
Compound: 6
Inhibition of DNP-BSA-induced degranulation in rat RBL2H3 cells assessed as reduction in beta-hexosaminidase release after 20 mins by spectrophotometry
Inhibition of DNP-BSA-induced degranulation in rat RBL2H3 cells assessed as reduction in beta-hexosaminidase release after 20 mins by spectrophotometry
[PMID: 22543029]
Sf21 IC50
>1000 μM
Compound: Ketotifen
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
[PMID: 21965623]
Sf21 IC50
>1 mM
Compound: Ketotifen
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
[PMID: 21965623]
Sf21 IC50
738.4 μM
Compound: Ketotifen
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
[PMID: 21965623]
体外実験

Ketotifen (0-100 μM; 2 or 4 days) inhibits SARS-CoV-2 with an EC50 of 48.9 μM; and increases the percentage inhibition of SARS-CoV-2 to 79%, 83% and 93% when co-administers with 25, 50 and 100 μM Indomethacin, respectively[3].
Ketotifen (0-50 μM; 24 h) has inhibitory activity against PR8, pH1N1 and H3N2 with EC50s of 5.9 μM, 33.7 μM and 48.5 μM, respectively; and exhibits relatively low cytotoxicity in MDCK cells (EC50=291 μM)[4].

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

Ketotifen 関連抗体
体内実験

Ketotifen (80 mg/kg; i.g.; daily for 3 days) reduces end organ damage and mortality in mice infected with influenza virus[4].
Ketotifen (0.4 mg/kg; i.p.; daily for 10 days) reduces encephalomyelitis (EAE) prevalence and severity[5].

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

Animal Model: Female C57BL/6 mice (4-6 weeks; intranasal infection with 1×103 TCID50 of PR8 in 30 μL of DMEM)[4]
Dosage: 80 mg/kg
Administration: i.g.; daily for 3 days
Result: Reduced end organ damage and mortality in infected mice.
Animal Model: Female C57BL/6 mice (5-6 weeks old; subcutaneously immunized with 150 μg of MOG35-55 peptide containing 4 mg/mL of Mycobacterium tuberculosis)[5]
Dosage: 0.4 mg/kg
Administration: i.p.; daily for 10 days (from the 7th day of infection)
Result: Reduced EAE prevalence and severity; reduced oxidative stress status and inflammasome activation at the CNS; reduced the amount of T cells, especially Th1, in the CNS; downregulated local mRNA expression for mast cell enzymes and preserves blood-CNS barrier permeability; triggered lymphocyte accumulation in draining lymph nodes.
臨床実験
分子量

309.43

分子式

C19H19NOS
CAS 番号
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(C1=C/2C=CS1)CC3=CC=CC=C3C2=C4CCN(C)CC/4
Structure Classification
Initial Source
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 : 10 mg/mL (32.32 mM; ultrasonic and warming and heat to 60°C; 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 3.2317 mL 16.1587 mL 32.3175 mL
5 mM 0.6463 mL 3.2317 mL 6.4635 mL
10 mM 0.3232 mL 1.6159 mL 3.2317 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)

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

    Solubility: ≥ 1 mg/mL (3.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (3.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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: 99.94%

COA (254 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, 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 3.2317 mL 16.1587 mL 32.3175 mL 80.7937 mL
5 mM 0.6463 mL 3.2317 mL 6.4635 mL 16.1587 mL
10 mM 0.3232 mL 1.6159 mL 3.2317 mL 8.0794 mL
15 mM 0.2154 mL 1.0772 mL 2.1545 mL 5.3862 mL
20 mM 0.1616 mL 0.8079 mL 1.6159 mL 4.0397 mL
25 mM 0.1293 mL 0.6463 mL 1.2927 mL 3.2317 mL
30 mM 0.1077 mL 0.5386 mL 1.0772 mL 2.6931 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Ketotifen 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:

Ketotifen34580-13-7HC 20-511Endogenous MetaboliteHistamine ReceptorSARS-CoVInfluenza VirusSARS coronavirusH1mast cellantiviralPR8pH1N1H3N2encephalomyelitisasthmaInhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
Ketotifen
製品番号:
HY-B0157
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.