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2g | ||
5g | ||
10g | ||
25g |
Azelastine (Allergodil) is a potent, second-generation, and selective histamine receptor antagonist, it is used in the treatment of rhinitis. Azelastine HCl has antiallergic effects related to histamine antagonism, and further antiallergic and anti-inflammatory effects unrelated to H1-receptor binding. Azelastine is shown to block secretion of IL-6, IL-8, and TNF alpha from mast cells by inhibiting NF-κB activation.
ln Vitro |
Inhibiting HNEpC proliferation greatly with ezelastine can aid in the fight against airway remodeling [5].
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ln Vivo |
In a rat model of diabetic hyperlipidemia Protein B, ezelastine (4 mg/kg; oral; daily; for 8 weeks) dramatically lowers serum alkaline phosphatase (ALP), osteocalcin, blood glucose, and HbA1c and downregulates lipopolysaccharide [2]. In a rat model of diabetic hyperlipidemia, ezelastine (4 mg/kg; oral; daily; for 8 weeks) improves the lipid profile (increasing HDL-c and lowering LDL-c) [2]. In a rat model of diabetic hyperlipidemia, ezelastine (4 mg/kg; oral; daily; for 8 weeks) decreases aortic calcification and calcium deposition [2].
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Cell Assay |
Cell proliferation assay [5]
Cell Types: Human nasal epithelial cells (HNEpC) Tested Concentrations: 100 μM, 400 μM Incubation Duration: 21 days Experimental Results: Inhibition of HNEpC growth. Western Blot Analysis[5] Cell Types: Human nasal epithelial cells (HNEpC) Tested Concentrations: 100 μM Incubation Duration: 7 days Experimental Results: H1R, M1R and M3R levels were Dramatically upregulated. |
Animal Protocol |
Animal/Disease Models: Male albino Wistar rat (150-170 g), diabetic hyperlipidemia rat model [2]
Doses: 4 mg/kg Route of Administration: Orally, one time/day for 8 weeks Experimental Results: Aortic calcification Improvement, apolipoprotein A expression increased, while apolipoprotein B diminished. |
References |
[1]. Craig La Force. Review of the pharmacology, clinical efficacy, and safety of azelastine hydrochloridel. Expert Rev Clin Immunol. 2005 Jul;1(2):191-201.
[2]. Mohamed M Elseweidy, et al. Azelastine a potent antihistamine agent, as hypolipidemic and modulator for aortic calcification in diabetic hyperlipidemic rats model. Arch Physiol Biochem. 2020 Jul 2;1-8. [3]. Carlos D. Zappia, et al. Azelastine potentiates antiasthmatic dexamethasone effect on a murine asthma model. Pharmacol Res Perspect. 2019 Dec; 7(6): e00531. [4]. Li Yang, et al. Identification of SARS-CoV-2 entry inhibitors among already approved drugs. Acta Pharmacol Sin. 2020 Oct 28 : 1-7. [5]. Shao-Cheng Liu, et al. Effect of budesonide and azelastine on histamine signaling regulation in human nasal epithelial cells. Eur Arch Otorhinolaryngol. 2017 Feb;274(2):845-853. |
Molecular Formula |
C₂₂H₂₄CLN₃O
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Molecular Weight |
381.90
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CAS # |
58581-89-8
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Related CAS # |
Azelastine hydrochloride;79307-93-0;Azelastine-13C,d3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1N(C2CCN(C)CCC2)N=C(CC3=CC=C(Cl)C=C3)C4=C1C=CC=C4
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Synonyms |
Allergodil Azelastine HCl Astelin Optivar Rhinolast Azeptin
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6185 mL | 13.0924 mL | 26.1849 mL | |
5 mM | 0.5237 mL | 2.6185 mL | 5.2370 mL | |
10 mM | 0.2618 mL | 1.3092 mL | 2.6185 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.