N-desmethyl Azelastine (Synonyms: DAZ, Desmethylazelastine) |
| Catalog No.GC52045 |
N-desmethyl Azelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours.
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Cas No.: 47491-38-3
Sample solution is provided at 25 µL, 10mM.
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N-desmethyl Azelastine is an active metabolite of the histamine H1 receptor antagonist azelastine .1,2 It is formed from azelastine primarily by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2D6 and, to a lesser extent, by CYP1A2.2 N-desmethyl Azelastine (1 µM) inhibits acetylcholine-induced depolarization and contractions in isolated human tracheal smooth muscle.1 It also inhibits transport of daunorubicin and digoxin in LLC-GA5-CoL150 cells overexpressing P-glycoprotein (P-gp), also known as multidrug resistance protein 1 (MDR1; IC50s = 11.8 and 41.8 µM, respectively).3
1.Richards, I.S., Miller, L., Solomon, D., et al.Azelastine and desmethylazelastine suppress acetylcholine-induced contraction and depolarization in human airway smooth muscleEur. J. Pharmacol.186(2-3)331-334(1990) 2.Nakajima, M., Nakamura, S., Tokudome, S., et al.Azelastine N-demethylation by cytochrome P-450 (CYP)3A4, CYP2D6, and CYP1A2 in human liver microsomes: Evaluation of approach to predict the contribution of multiple CYPsDrug Metab. Dispos.27(12)1381-1391(1999) 3.Katoh, M., Nakajima, M., Yamazaki, H., et al.Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transportEur. J. Pharm. Sci.12(4)505-513(2001)
| Cas No. | 47491-38-3 | SDF | |
| Synonyms | DAZ, Desmethylazelastine | ||
| Canonical SMILES | O=C1C2=CC=CC=C2C(CC3=CC=C(Cl)C=C3)=NN1C4CCNCCC4 | ||
| Formula | C21H22ClN3O | M.Wt | 367.9 |
| Solubility | DMSO: soluble | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7181 mL | 13.5906 mL | 27.1813 mL |
| 5 mM | 0.5436 mL | 2.7181 mL | 5.4363 mL |
| 10 mM | 0.2718 mL | 1.3591 mL | 2.7181 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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