Ebastine

製品コードS4262 バッチS426202

印刷

化学情報

Synonyms

LAS-W 090,RP64305

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₂H₃₉NO₂

分子量

469.66

CAS No.

90729-43-4

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

93 mg/mL (198.01 mM)

Ethanol

93 mg/mL (198.01 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Ebastine(LAS-W 090,RP64305) is a potent H1-histamine receptor antagonist, used for allergic disorders.
in vitro	Ebastine at concentrations approximating those found in plasma under certain conditions suppresses in a voltage-independent manner the I(Kr) (Kd = 0.14 μM, maximum block 74%) more effectively than the slowly delayed rectifier K+ current (I(Ks)) (Kd = 0.8 μM, maximum block 60%) in guinea pig ventricular myocytes. This compound also suppresses IKr in HERG-expressing X. laevis oocytes with the K d value of 0.3 μM and a maximal block of 46% at 3 μM. It produces negligible effect on rat transient K+ current at concentrations of <100 nM. ^[1] This chemical is shown to block the release of anti-IgE-induced prostaglandin D2 (PGD2) and leukotriene C4/D4 from human nasal polyp cells (IC30 values of 2.57 and 9.6 μM, respectively) and to inhibit the release of cytokines. ^[2] It is a novel histamine H1 receptor antagonist that combines potency with a rapid onset (fast absorption) and long duration (slow elimination) of action, at least partially mediated via the formation of an acid metabolite (carebastine) that is even more potent as an antihistamine. This agent has negligible activity against acetylcholine (no atropine-like adverse effects on secretions and visual accommodation) and only poorly penetrates the blood-brain barrier (no sedative adverse effects). It is without effects on the central nervous and cardiovascular systems, even after oral administration of high doses, and does not interact pharmacologically with a wide range of other drugs covering most areas of potential coadministration. This compound shows clear selectivity for histamine H1 as opposed to H2 receptors, has moderate activity against other potential mediators of allergic phenomena such as leukotriene C4 and platelet-activating factor, and is clearly effective against anaphylactic reactions resulting from exposure of suitably sensitised tissues or animals to antigen. ^[3]

製品説明

Ebastine(LAS-W 090,RP64305) is a potent H1-histamine receptor antagonist, used for allergic disorders.

in vitro

Ebastine at concentrations approximating those found in plasma under certain conditions suppresses in a voltage-independent manner the I(Kr) (Kd = 0.14 μM, maximum block 74%) more effectively than the slowly delayed rectifier K+ current (I(Ks)) (Kd = 0.8 μM, maximum block 60%) in guinea pig ventricular myocytes. This compound also suppresses IKr in HERG-expressing X. laevis oocytes with the K d value of 0.3 μM and a maximal block of 46% at 3 μM. It produces negligible effect on rat transient K+ current at concentrations of <100 nM. ^[1] This chemical is shown to block the release of anti-IgE-induced prostaglandin D2 (PGD2) and leukotriene C4/D4 from human nasal polyp cells (IC30 values of 2.57 and 9.6 μM, respectively) and to inhibit the release of cytokines. ^[2] It is a novel histamine H1 receptor antagonist that combines potency with a rapid onset (fast absorption) and long duration (slow elimination) of action, at least partially mediated via the formation of an acid metabolite (carebastine) that is even more potent as an antihistamine. This agent has negligible activity against acetylcholine (no atropine-like adverse effects on secretions and visual accommodation) and only poorly penetrates the blood-brain barrier (no sedative adverse effects). It is without effects on the central nervous and cardiovascular systems, even after oral administration of high doses, and does not interact pharmacologically with a wide range of other drugs covering most areas of potential coadministration. This compound shows clear selectivity for histamine H1 as opposed to H2 receptors, has moderate activity against other potential mediators of allergic phenomena such as leukotriene C4 and platelet-activating factor, and is clearly effective against anaphylactic reactions resulting from exposure of suitably sensitised tissues or animals to antigen. ^[3]

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/9103502/
https://pubmed.ncbi.nlm.nih.gov/8983912/
https://pubmed.ncbi.nlm.nih.gov/8828021/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Mast cell activation triggered by SARS-CoV-2 causes inflammation in brain microvascular endothelial cells and microglia [ Front Cell Infect Microbiol, 2024, 14:1358873]	PubMed: 38638822
Mast cell activation triggered by SARS-CoV-2 causes inflammation in brain microvascular endothelial cells and microglia [ Front Cell Infect Microbiol, 2024, 14:1358873]	PubMed: 38638822
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization [ Cell Rep Methods, 2023, 3(10):100599]	PubMed: 37797618
Combinational benefit of antihistamines and remdesivir for reducing SARS-CoV-2 replication and alleviating inflammation-induced lung injury in mice [ Zool Res, 2022, 43(3):457-468]	PubMed: 35503561
SARS-CoV-2-triggered mast cell rapid degranulation induces alveolar epithelial inflammation and lung injury [ Signal Transduct Target Ther, 2021, 6(1):428]	PubMed: 34921131

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。