| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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Purity: ≥98%
Azelastine HCl (Allergodil; Astelin; Optivar; Rhinolast; Azeptin), the hydrochloride salt of azelastine, is a potent, 2nd-generation, and selective histamine receptor antagonist used for the treatment of rhinitis. In addition to its antiallergic and anti-inflammatory properties unrelated to H1-receptor binding, azelastine HCl exhibits antiallergic effects linked to histamine antagonism. Azelastine has been demonstrated to prevent mast cell production of TNF alpha, IL-6, and IL-8 by preventing NF-κB activation.
| Targets |
H1 Receptor
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|---|---|---|
| ln Vitro |
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| ln Vivo |
Azelastine hydrochloride (4 mg/kg; p.o.; daily; for 8 weeks) (4 mg/kg; p.o.; daily; for 8 weeks) significantly lowers blood glucose, HbA1c, serum alkaline phosphatase (ALP), osteocalcin, and 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) reduces calcium deposition and aortic calcification in diabetic hyperlipidemic rats model[2]. |
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| Cell Assay |
Cell Line: Human nasal epithelial cells (HNEpC)
Concentration: 100 μM, 400 μM Incubation Time: 21 days Result: Inhibited HNEpC growth. |
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| Animal Protocol |
Male albino Wistar rats (150-170 g), diabetic hyperlipidemic rats model
4 mg/kg Oral administration, daily, for 8 weeks |
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| References |
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| Additional Infomation |
Azelastine hydrochloride is the hydrochloride salt of azelastine. It has a role as a platelet aggregation inhibitor, a bronchodilator agent, an anti-asthmatic drug, an anti-allergic agent, a H1-receptor antagonist and an EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor. It contains an azelastine.
Azelastine Hydrochloride is the hydrochloride salt form of azelastine, a phthalazinone derivative with antihistaminergic activity. Azelastine hydrochloride competes with histamine for the H1 receptor, thereby diminishing the actions of histamine on effector cells and decreasing the histamine-mediated symptoms of allergic reaction, such as bronchoconstriction, vasodilation, increased capillary permeability and spasmodic contractions of gastrointestinal smooth muscle. See also: Azelastine (has active moiety); Azelastine hydrochloride; fluticasone propionate (component of). |
| Molecular Formula |
C22H25CL2N3O
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|---|---|---|
| Molecular Weight |
418.36
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| Exact Mass |
417.137
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| Elemental Analysis |
C, 63.16; H, 6.02; Cl, 16.95; N, 10.04; O, 3.82
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| CAS # |
79307-93-0
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| Related CAS # |
Azelastine; 58581-89-8; Azelastine-13C,d3 hydrochloride
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| PubChem CID |
54360
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| Appearance |
White to off-white solid powder
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| Density |
1.25 g/cm3
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| Boiling Point |
533.9ºC at 760 mmHg
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| Melting Point |
225-229ºC
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| Flash Point |
276.7ºC
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| LogP |
5.037
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
558
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.O=C1N(C2CCCN(C)CC2)N=C(CC2C=CC(Cl)=CC=2)C2C1=CC=CC=2
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| InChi Key |
YEJAJYAHJQIWNU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H24ClN3O.ClH/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16;/h2-3,6-11,18H,4-5,12-15H2,1H3;1H
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| Chemical Name |
4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one;hydrochloride
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| Synonyms |
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06008860 | Recruiting | Drug: Experimental: Primary Cohort Other: Placebo Comparator: Primary Cohort - Placebo |
COVID-19 | University of Chicago | July 1, 2023 | Phase 4 |
| NCT06126952 | Recruiting | Drug: Treatment A: Azelastine hydrochloride 0.15% nasal spray Drug: Treatment B: Placebo (Azelastine 0.15% vehicle) nasal spray |
Seasonal Allergic Rhinitis |
MEDA Pharma GmbH & Co. KG | October 30, 2023 | Phase 2 |
| NCT05626621 | Recruiting | Drug: Mometasone (1 mg) and Azelastine (1 mg) Nasal Irrigation Drug: Mometasone Nasal Irrigation (1 mg capsule) |
Chronic Rhinitis | NorthShore University HealthSystem |
November 23, 2022 | Phase 4 |
| NCT04264637 | Completed | Drug: Azelastine hydrochloride (BAYR9258) Drug: Placebo |
Allergic Rhinitis | Bayer | February 3, 2020 | Phase 3 |
| NCT00612118 | Recruiting | Drug: azelastine hydrochloride Drug: GSK256066 |
Rhinitis, Allergic, Seasonal Allergic Rhinitis |
GlaxoSmithKline | February 2008 | Phase 2 |
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