Cetirizine dihydrochloride 是羟嗪的羧化代谢物,是第二代抗组胺药。Cetirizine dihydrochloride 是一种特异的、口服有效的、H1 受体的长效拮抗剂。Cetirizine dihydrochloride 标记抗过敏特性,抑制过敏反应期间嗜酸性粒细胞趋化。
生物活性 | Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamineH1-receptorantagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3]. |
体外研究 (In Vitro) | Cetirizine (>5 μM) at higher concentrations can reduce the release of GM-CSF and IL-8 from A549 cells stimulated with IL-1β. Cetirizine exerts anti-inflammatory effects beyond histamine H1-receptor antagonist[2].
Cell Viability Assay[2] Cell Line: | Human airway epithelial cell line A549. | Concentration: | 0-10 μM. | Incubation Time: | 24 h. | Result: | The survival of A549 cells incubated with various concentrations of cetirizine (0.1, 1, 2.5, 5, and 10 μM) for 24 hours were all higher than 90% when comparing with the control group by MTT test. Cetirizine, 5 and 10 μM, suppressed GM-CSF release by 70.71 and 61.55%, respectively. Preincubation with cetirizine, 10 μM, suppressed the IL-8 secretion by 75.04%. |
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体内研究 (In Vivo) | Cetirizine (20 mg/kg, mice, orally) exerts its anti-inflammatory effects by inhibiting MIF as well as IL-8 production in mice immunized and challenged with ragweed pollen[3].
Animal Model: | Male 8-week-old BALB/c mice (25-30 g) immunized and challenged with ragweed pollen[3]. | Dosage: | 2 or 20 mg/kg. | Administration: | Orally, diluted in sterile water on days 18, 19, and 20. | Result: | The neutrophilia at 8 h and eosinophilia at 24 h induced by ragweed pollen extract per os
were significantly reduced in the mice treated with 20 mg/kg. The dosage with 2 mg/kg had no effect. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(216.54 mM;Need ultrasonic) H2O : 100 mg/mL(216.54 mM;Need ultrasonic) 配制储备液 1 mM | 2.1654 mL | 10.8270 mL | 21.6539 mL | 5 mM | 0.4331 mL | 2.1654 mL | 4.3308 mL | 10 mM | 0.2165 mL | 1.0827 mL | 2.1654 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 120 mg/mL (259.85 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.41 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.41 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.41 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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