2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Ebastine

エバスチン  (Synonyms: Ebastine; LAS-W 090; RP64305)

製品番号: HY-B0674 純度: 99.95%
COA 取扱説明書 Technical Support

Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research.

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Ebastine

エバスチン 構造式

CAS 番号 : 90729-43-4

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 66 在庫あり
Solution
10 mM * 1 mL in DMSO USD 66 在庫あり
Solid
500 mg $60 在庫あり
1 g $84 在庫あり
5 g $250 在庫あり
10 g   お問い合わせ  
50 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

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

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of Ebastine:

エバスチン 関連抗体

Top Publications Citing Use of Products

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

Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research[1].

IC50 & Target[1]

H1 Receptor

 

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
9.56 μM
Compound: Ebastine
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
[PMID: 29624387]
Vero CC50
15.42 μM
Compound: Ebastine
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
10.1101/2020.03.20.999730
Vero IC50
6.92 μM
Compound: Ebastine
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
10.1101/2020.03.20.999730
体外実験

Ebastine (10-500 ng/mL; 24-48 hours) treatment significantly increases the proliferation of HFDPC[2].
Ebastine (10-500 ng/mL; 24-48 hours) treatment shows dose-dependent increases in Cyclin D1, Cyclin E1, and Cyclin A expression levels. And the expression levels of Cdk4, Cdk2, and Cdc2 are alos increased. Ebastine treatment elevates expression levels of phospho-AKT and phospho-p44/42 extracellular signal-regulated kinase[2].

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

エバスチン 関連抗体

Cell Proliferation Assay[2]

Cell Line: Human follicle dermal papilla cells (HFDPC)
Concentration: 10 ng/mL, 50 ng/mL, 100 ng/mL, 200 ng/mL, 500 ng/mL
Incubation Time: 24 hours, 48 hours
Result: The proliferative activity in cells was significantly enhanced.

Western Blot Analysis[2]

Cell Line: Human follicle dermal papilla cells (HFDPC)
Concentration: 10 ng/mL, 50 ng/mL, 100 ng/mL, 200 ng/mL, 500 ng/mL
Incubation Time: 24 hours
Result: The expression levels of cell-cycle regulatory proteins and an antiapoptotic protein were increased in HFDPC.
体内実験

In rats, after intravenous administration of [14C]Ebastine at 2 mg/kg, the plasma level of radioactivity decreased biphasically with α-phase half-life (t1/2 α) of 1.6 h and β-phase half-life (t1/2 β) of 3.1 h[3].
Following oral administration of [14C]Ebastine at a dose of 2 mg/kg, the plasma level reached the maximum (Cmax) of 102 ng eq./ml at 2 h and decreased monophasically with t1/2 of 3.9 h. At 20 mg/kg, a monophasic decrease is also observed with Cmax of 1110 ng eq./ml at 4 h and with t1/2 of 4.0 h[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

469.66

分子式

C32H39NO2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C(C)(C)C)C=C1)CCCN2CCC(OC(C3=CC=CC=C3)C4=CC=CC=C4)CC2
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: 

Ethanol : 58.75 mg/mL (125.09 mM; Need ultrasonic)

DMSO : 8.33 mg/mL (17.74 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 2.1292 mL 10.6460 mL 21.2920 mL
5 mM 0.4258 mL 2.1292 mL 4.2584 mL
10 mM 0.2129 mL 1.0646 mL 2.1292 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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.83 mg/mL (1.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (1.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: 99.95%

COA (245 KB) HNMR (171 KB) RP-HPLC (255 KB) MS (68 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 / Ethanol 1 mM 2.1292 mL 10.6460 mL 21.2920 mL 53.2300 mL
5 mM 0.4258 mL 2.1292 mL 4.2584 mL 10.6460 mL
10 mM 0.2129 mL 1.0646 mL 2.1292 mL 5.3230 mL
15 mM 0.1419 mL 0.7097 mL 1.4195 mL 3.5487 mL
Ethanol 20 mM 0.1065 mL 0.5323 mL 1.0646 mL 2.6615 mL
25 mM 0.0852 mL 0.4258 mL 0.8517 mL 2.1292 mL
30 mM 0.0710 mL 0.3549 mL 0.7097 mL 1.7743 mL
40 mM 0.0532 mL 0.2661 mL 0.5323 mL 1.3307 mL
50 mM 0.0426 mL 0.2129 mL 0.4258 mL 1.0646 mL
60 mM 0.0355 mL 0.1774 mL 0.3549 mL 0.8872 mL
80 mM 0.0266 mL 0.1331 mL 0.2661 mL 0.6654 mL
100 mM 0.0213 mL 0.1065 mL 0.2129 mL 0.5323 mL
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Ebastine 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:

Ebastine90729-43-4LAS-W 090 RP64305RP64305RP 64305RP-64305Histamine ReceptorantihistamineantiallergicallergicrhinitisidiopathicurticariaInhibitorinhibitorinhibit

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Ebastine
製品番号:
HY-B0674
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