WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H317302
CAS#: 79307-93-0
Description: Azelastine HCl is a potent and selective H1-receptor antagonist, with antiallergic effects related to histamine antagonism, and further antiallergic and anti-inflammatory effects unrelated to H1-receptor binding. Azelastine HCl is an activator of NF-kB activator. Azelastine hydrochloride has been used in a study to investigate the potential of polymeric microspheres for treatment of allergic conjunctivitis. Azelastine is shown to block secretion of IL-6, IL-8, and TNF alpha from mast cells by inhibiting NF-κB activation.
Hodoodo Cat#: H317302
Name: Azelastine HCl
CAS#: 79307-93-0
Chemical Formula: C22H25Cl2N3O
Exact Mass: 0.00
Molecular Weight: 418.360
Elemental Analysis: C, 63.16; H, 6.02; Cl, 16.95; N, 10.04; O, 3.82
Synonym: Azelastine HCl; Astelin; Optivar; Allergodil; Rhinolast; Azeptin
IUPAC/Chemical Name: 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one;hydrochloride
InChi Key: YEJAJYAHJQIWNU-UHFFFAOYSA-N
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
SMILES Code: CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl.Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | Azelastine hydrochloridem, an antihistamine, is a potent and selective histamine 1 (H1) antagonist. |
| In vitro activity: | HT29, DLD1, and HCT116 cells were exposed to different azelastine concentrations for up to 72 h followed by the WST-1 assay. As displayed in Figure 1C, CRC cell viability was significantly reduced with increasing concentration of azelastine. Besides, azelastine significantly decreased both anchorage-dependent and -independent colony formation abilities of CRC cells, as determined by the colony formation and soft agar assays (Figure S1A-B). The annexin V-FITC/PI double-staining assay was used to analyze azelastine's effect on apoptosis. The results indicated apoptosis induction in a dose-dependent manner in HT29, DLD1, and HCT116 cells (Figure 1D), which was also confirmed by the increased cleaved caspase-3 expression upon azelastine treatment (Figure 1E). Reference: Theranostics. 2021; 11(4): 1828–1844. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7778598/ |
| In vivo activity: | Azelastine significantly reduced blood glucose, HbA1c and serum ALP, OCN, downregulated apo B, improved the lipid profile (LDL-c decrease and HDL-c increase), attenuated calcium deposition and aortic calcification as compared to control rat group. Reference: Arch Physiol Biochem. 2020 Jul 2:1-8. https://pubmed.ncbi.nlm.nih.gov/32615812/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48.0 | 114.73 | |
| DMSO:PBS (pH 7.2) (1:3) | 0.3 | 0.60 | |
| DMF | 1.0 | 2.39 | |
| Ethanol | 24.1 | 100.69 | |
| Water | 20.8 | 49.81 |
The following data is based on the product molecular weight 418.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Ge S, Lu J, Hou Y, Lv Y, Wang C, He H. Azelastine inhibits viropexis of SARS-CoV-2 spike pseudovirus by binding to SARS-CoV-2 entry receptor ACE2. Virology. 2021 Aug;560:110-115. doi: 10.1016/j.virol.2021.05.009. Epub 2021 May 25. PMID: 34052578; PMCID: PMC8144927. 2. Hu HF, Xu WW, Li YJ, He Y, Zhang WX, Liao L, Zhang QH, Han L, Yin XF, Zhao XX, Pan YL, Li B, He QY. Anti-allergic drug azelastine suppresses colon tumorigenesis by directly targeting ARF1 to inhibit IQGAP1-ERK-Drp1-mediated mitochondrial fission. Theranostics. 2021 Jan 1;11(4):1828-1844. doi: 10.7150/thno.48698. PMID: 33408784; PMCID: PMC7778598. 3. Elseweidy MM, Elnagar GM, Elsawy MM, Zein N. 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. doi: 10.1080/13813455.2020.1786129. Epub ahead of print. PMID: 32615812. |
| In vitro protocol: | 1. Ge S, Lu J, Hou Y, Lv Y, Wang C, He H. Azelastine inhibits viropexis of SARS-CoV-2 spike pseudovirus by binding to SARS-CoV-2 entry receptor ACE2. Virology. 2021 Aug;560:110-115. doi: 10.1016/j.virol.2021.05.009. Epub 2021 May 25. PMID: 34052578; PMCID: PMC8144927. 2. Hu HF, Xu WW, Li YJ, He Y, Zhang WX, Liao L, Zhang QH, Han L, Yin XF, Zhao XX, Pan YL, Li B, He QY. Anti-allergic drug azelastine suppresses colon tumorigenesis by directly targeting ARF1 to inhibit IQGAP1-ERK-Drp1-mediated mitochondrial fission. Theranostics. 2021 Jan 1;11(4):1828-1844. doi: 10.7150/thno.48698. PMID: 33408784; PMCID: PMC7778598. |
| In vivo protocol: | 1. Elseweidy MM, Elnagar GM, Elsawy MM, Zein N. 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. doi: 10.1080/13813455.2020.1786129. Epub ahead of print. PMID: 32615812. 2. Hu HF, Xu WW, Li YJ, He Y, Zhang WX, Liao L, Zhang QH, Han L, Yin XF, Zhao XX, Pan YL, Li B, He QY. Anti-allergic drug azelastine suppresses colon tumorigenesis by directly targeting ARF1 to inhibit IQGAP1-ERK-Drp1-mediated mitochondrial fission. Theranostics. 2021 Jan 1;11(4):1828-1844. doi: 10.7150/thno.48698. PMID: 33408784; PMCID: PMC7778598. |
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