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Ebastine
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很棒纯度: 99.99%
货号 T2335Cas号 90729-43-4
别名 依巴斯汀, RP64305, LAS-W 090, Kestine, Ebastin, Ebastel
Ebastine (Kestine) 是一种可口服的组胺 H1 受体拮抗剂，用于过敏性鼻炎的症状和慢性特发性荨麻疹的研究。
其他形式的 “Ebastine”:
Ebastine
一键复制产品信息 很棒纯度: 99.99%
货号 T2335 别名 依巴斯汀, RP64305, LAS-W 090, Kestine, Ebastin, EbastelCas号 90729-43-4
Ebastine (Kestine) 是一种可口服的组胺 H1 受体拮抗剂，用于过敏性鼻炎的症状和慢性特发性荨麻疹的研究。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 200 mg | ¥ 99 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 195 | 现货 |
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产品介绍
Ebastine AI Summary
Ebastine exhibits a broad spectrum of bioactivities interacting with multiple cellular targets and pathways. It demonstrates significant receptor binding with H1, Alpha-1 adrenergic, 5-hydroxytryptamine 1A, and Dopamine D2 receptors, showing a dissociation constant (KD) of 4.0 nM, and displaying a logP value of 2.74. The compound provides protective effects against histamine-induced lethality in guinea pigs and demonstrates inhibition of efflux pumps, including human recombinant MDR1 and norA-mediated ethidium bromide efflux, with inhibition rates of 99.0% and 88.3% respectively.
Ebastine inhibits the potassium channel HERG (IC50 = 3019.95 nM) and shows inhibition of the MES-SA/DX5 cell line through a P-glycoprotein assay with activity level 1.76. It has a wide range of receptor binding affinities, including moderate binding to Adenosine A3 and Alpha-2 adrenergic receptors, and inhibition of Calcium Channel Type L. Additionally, it has varying affinities with Dopamine receptors (D1, D2L, D3, D4.2), Histamine, Muscarinic, Serotonin, Potassium, Protein Tyrosine Kinase, Sigma, Sodium, and Tachykinin NK2 receptors.
Its antiviral activities are notable, demonstrating inhibition against SARS-CoV-2 (IC50 of 6920.0 nM) and showing moderate cytotoxicity in Vero cells (CC50 of 15420.0 nM). Ebastine exhibits antiviral actions by inhibiting SARS-CoV-2 induced cytotoxicity and viral entry in human and VERO-6 cells. It also shows inhibition of the SARS-CoV-2 3CL-Pro protease and potential effects against Ebolavirus.
Moreover, Ebastine inhibits human HDAC6 and shows inhibition of DGKalpha activity. Despite its broad bioactivity, it does not significantly inhibit human BSEP, MRP2, MRP3, and MRP4 transporters. The compound affects various biomarkers related to liver and kidney function, blood chemistry, enzyme levels, mineral levels, cholesterol levels, and blood cell counts.
Overall, Ebastine is a versatile candidate for further research due to its wide range of bioactivities, including receptor binding affinity, inhibition of efflux pumps, antiviral properties, and interactions with multiple cellular targets..
Note: Summary generated by AI. Data source: ChEMBL 
生物活性
化学信息
储存&溶解度
| 产品描述 | Ebastine (Kestine) (trade names Evastin, Kestine, Ebastel, Aleva) is a non-sedating H1 antihistamine. It does not penetrate the blood-brain barrier and thus allows an effective block of the H1 receptor in peripheral tissue without a central side effect, i. e not causing sedation or drowsiness. |
| 体内活性 | 相较于于H2受体,Ebastine显示对组胺H1的选择性,对过敏现象的其他潜在介质如白三烯C4和血小板活化因子具有中等活性,并且显然有效地针对由适当敏化的组织或动物暴露于过敏引起的过敏反应抗原。Ebastine在人鼻息肉细胞中,抑制抗IgE诱导的前列腺素D2和白三烯C4/D4的释放,IC30分别是2.57 μM和9.6 μM,并抑制细胞因子的释放。Ebastine也抑制hERG表达非洲爪蟾卵母细胞的IKr,Kd值为0.3 μM,在3 μM时的最大抑制率为46%。Ebastine在浓度小于100 nM时对大鼠瞬时钾电流产生微小的影响。 |
| 别名 | 依巴斯汀, RP64305, LAS-W 090, Kestine, Ebastin, Ebastel |
| 分子量 | 469.66 |
| 分子式 | C32H39NO2 |
| CAS No. | 90729-43-4 |
| Smiles | C(OC1CCN(CCCC(=O)C2=CC=C(C(C)(C)C)C=C2)CC1)(C3=CC=CC=C3)C4=CC=CC=C4 |
| 密度 | 1.09 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| 溶解度信息 | DMSO: 4.7 mg/mL (10.01 mM), Sonication is recommended.  | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
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计算器
体内实验配液计算器
请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：
比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL， 一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O， 那么您的工作液浓度为2 mg/mL。
母液配置方法：2 mg 药物溶于 100 μL DMSO （ 母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。
体内配方的制备方法： 取 100 μL DMSO 母液， 添加 400 μL PEG300 混匀澄清， 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。
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