盐酸西替利嗪作用机制 - Medchemexpress - MCE中国

1、Product Data SheetCetirizine dihydrochlorideCat. No.: HY-17042ACAS No.: 83881-52-1分式: CHClNO分量: 461.81作靶点: Histamine Receptor作通路: GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (216.54 mM; Ne

2、ed ultrasonic)H2O : 100 mg/mL (216.54 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.1654 mL 10.8270 mL 21.6539 mL5 mM 0.4331 mL 2.1654 mL 4.3308 mL10 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 mont

3、h。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 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 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.41 mM

4、); Clear solution此案可获得 2.5 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.41 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg

5、/mL (5.41 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.41 mM); Clear solution此案可获得 2.5 mg/mL (5.41 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。B

6、IOLOGICAL ACTIVITY物活性 Cetirizine dihydrochloride羟嗪的羧化代谢物， 第代抗组胺药。Cetirizine dihydrochloride 种特异的、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。体外研究 Cetirizine (5 M) at higher concentrations can reduce the release of GM-CSF and IL-8 from A549 cells stimulatedwith IL-1. Cetiriz

7、ine exerts anti-inflammatory effects beyond histamine H1-receptor antagonist2.Cell Viability Assay2Cell Line: Human airway epithelial cell line A549.Concentration: 0-10 M.Incubation Time: 24 h.Result: The survival of A549 cells incubated with various concentrations of cetirizine (0.1, 1, 2.5, 5, and

8、 10 M) for 24 hours were all higher than 90% when comparing with the control group by MTT test.Cetirizine, 5 and 10 M, suppressed GM-CSF release by 70.71 and 61.55%, respectively.Preincubation with cetirizine, 10 M, suppressed the IL-8 secretion by 75.04%.体内研究 Cetirizine (20 mg/kg, mice, orally) exe

9、rts its anti-inflammatory effects by inhibiting MIF as well as IL-8 production inmice immunized and challenged with ragweed pollen3.Animal Model: Male 8-week-old BALB/c mice (25-30 g) immunized and challenged with ragweed pollen3.Dosage: 2 or 20 mg/kg.Administration: Orally, diluted in sterile water

10、 on days 18, 19, and 20.Result: The neutrophilia at 8 h and eosinophilia at 24 h induced by ragweed pollen extract per oswere significantly reduced in themice treated with 20 mg/kg. The dosage with 2 mg/kg had no effect.户使本产品发表的科研献 Pharmacol Res. 2017 Nov;125(Pt B):150-160.See more customer validati

11、ons on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Caroline M. Spencer, et al. Cetirizine. Drugs 46 (6): 10551080, 1993.Page 2 of 3 www.MedChemE2. Shih MY, et al. Influence of cetirizine and levocetirizine on two cytokines secretion in human airway epithelial cells. Allergy Asthma Proc. 2008 Sep-Oct;29(5):480-5.3. Shimizu T, et al. Cetirizine, an H1-receptor antagonist, suppresses the expression of macrophage migration inhibitory factor: its potential anti-inflammatory action. Clin Exp Allergy. 2004 Jan;34(1):103-9.McePdfHeightCaution: Product has not been full