Azelastine hydrochloride

Name: Azelastine hydrochloride
Brand: MedChemExpress
SKU: HY-B0462
Rating: 4.5 (1 reviews)

Cat. No.: HY-B0462 Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Azelastine hydrochloridem, an antihistamine, is a potent and selective histamine 1 (H₁) antagonist. Azelastine hydrochloride can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2.

For research use only. We do not sell to patients.

Azelastine hydrochloride Chemical Structure

CAS No. : 79307-93-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 69	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Azelastine hydrochloride:

Azelastine Get quote
Azelastine-¹³C,d₃ hydrochloride Get quote

1 Publications Citing Use of MCE Azelastine hydrochloride

•Phytomedicine. 2023 Apr 21, 154825.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

H₁ Receptor

In Vitro

Azelastine hydrochloride can significantly inhibit HNEpC proliferation, and therefore, be helpful in against airway remodeling^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

Molecular Weight

418.36

Formula

C₂₂H₂₅Cl₂N₃O

CAS No.

79307-93-0

Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C2CCN(C)CCC2)N=C(CC3=CC=C(Cl)C=C3)C4=C1C=CC=C4.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (119.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 6.67 mg/mL (15.94 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (280 KB) SDS (392 KB)

COA (252 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[3]. Carlos D. Zappia, et al. Azelastine potentiates antiasthmatic dexamethasone effect on a murine asthma model. Pharmacol Res Perspect. 2019 Dec; 7(6): e00531. [Content Brief]

[4]. Li Yang, et al. Identification of SARS-CoV-2 entry inhibitors among already approved drugs. Acta Pharmacol Sin. 2020 Oct 28 : 1–7. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.3903 mL	11.9514 mL	23.9029 mL	59.7571 mL
	5 mM	0.4781 mL	2.3903 mL	4.7806 mL	11.9514 mL
	10 mM	0.2390 mL	1.1951 mL	2.3903 mL	5.9757 mL
	15 mM	0.1594 mL	0.7968 mL	1.5935 mL	3.9838 mL
DMSO	20 mM	0.1195 mL	0.5976 mL	1.1951 mL	2.9879 mL
	25 mM	0.0956 mL	0.4781 mL	0.9561 mL	2.3903 mL
	30 mM	0.0797 mL	0.3984 mL	0.7968 mL	1.9919 mL
	40 mM	0.0598 mL	0.2988 mL	0.5976 mL	1.4939 mL
	50 mM	0.0478 mL	0.2390 mL	0.4781 mL	1.1951 mL
	60 mM	0.0398 mL	0.1992 mL	0.3984 mL	0.9960 mL
	80 mM	0.0299 mL	0.1494 mL	0.2988 mL	0.7470 mL
	100 mM	0.0239 mL	0.1195 mL	0.2390 mL	0.5976 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.