Azelastine hydrochloride 属于抗组胺剂，是一种有效的选择性组胺 1 (H1) 拮抗剂。Azelastine hydrochloride 可用于过敏性鼻炎、哮喘、糖尿病高脂血症和 SARS-CoV-2 的研究。
| 生物活性 | Azelastine hydrochloridem, an antihistamine, is a potent and selectivehistamine 1 (H1)antagonist. Azelastine hydrochloride can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4]. |
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体外研究
(In Vitro) | Azelastine hydrochloride can significantly inhibit HNEpC proliferation, and therefore, be helpful in against airway remodeling[5].
Cell Proliferation Assay[5] | Cell Line: | Human nasal epithelial cells (HNEpC) | | Concentration: | 100 μM, 400 μM | | Incubation Time: | 21 days | | Result: | Inhibited HNEpC growth. |
Western Blot Analysis[5] | Cell Line: | Human nasal epithelial cells (HNEpC) | | Concentration: | 100 μM | | Incubation Time: | 7 days | | Result: | Significantly up-regulated the H1R, M1R and M3R levels. |
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体内研究
(In Vivo) | Azelastine hydrochloride (4 mg/kg; p.o.; daily; for 8 weeks) significantly reduces blood glucose, HbA1c and serum alkaline phosphatase (ALP), osteocalcin and downregulates apolipoprotein B in diabetic hyperlipidemic rats model[2].
Azelastine hydrochloride (4 mg/kg; p.o.; daily; for 8 weeks) improves the lipid profile (LDL-c decrease and HDL-c increase) in diabetic hyperlipidemic rats model[2].
Azelastine hydrochloride (4 mg/kg; p.o.; daily; for 8 weeks) attenuates calcium deposition and aortic calcification in diabetic hyperlipidemic rats model[2].
| Animal Model: | Male albino Wistar rats (150-170 g), diabetic hyperlipidemic rats model[2] | | Dosage: | 4 mg/kg | | Administration: | Oral administration, daily, for 8 weeks | | Result: | Ameliorated aortic calcification and increased apolipoprotein A expression along with a decline in apolipoprotein B. |
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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 : 50 mg/mL(119.51 mM;Need ultrasonic) H2O : 6.67 mg/mL(15.94 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.3903 mL | 11.9514 mL | 23.9029 mL | | 5 mM | 0.4781 mL | 2.3903 mL | 4.7806 mL | | 10 mM | 0.2390 mL | 1.1951 mL | 2.3903 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： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.98 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.98 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.98 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.98 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。 *以上所有助溶剂都可在本网站选购。
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