Bilastine
Based on 1 Customer Validation
Bilastine is an oral histamine H1-receptor antagonist. Bilastine can be used for allergic rhinitis and urticaria studies, and it also improves diabetic nephropathy in mice, showing safety for the central nervous system.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 202189-78-4
- Formula: C28H37N3O3
- Molecular Weight:463.61
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Histamine Receptor Isoforms
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Biological Activity
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H1 Receptor |
Bilastine (1-30 mg/kg, i.g., once a day, for 14 weeks) preserves the integrity of glomerular connections in diabetic mice and improves diabetic nephropathy[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Beagle dogs, Wistar rats, CD1 mice[2]
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Dosage:0, 20, 125, 800 mg/kg for 8 and 52 weeks; 0, 200, 1000, 2000 mg/kg for 13 weeks; 0, 500, 1000, 2000 mg/kg for 13 weeks; daily
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Administration:i.g.
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Result:Was not associated with any mortality, ocular effects, or nodules/masses.
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Animal Model:Streptozotocin-induced diabetic mouse model[3]
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Dosage:1, 3, 10, 30 mg/kg; daily; 14 weeks
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Administration:i.g.
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Result:Prevented ACR increase and restored creatinine clearance, had a positive effect on glomerular filtration, and joint integrity was intact.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 202189-78-4
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Appearance Solid
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Molecular Weight 463.61
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Formula C28H37N3O3
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Color White to off-white
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SMILES
CC(C)(C1=CC=C(CCN2CCC(C3=NC4=CC=CC=C4N3CCOCC)CC2)C=C1)C(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 12.5 mg/mL (26.96 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.70 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.70 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. C. Bachert, et al. Bilastine in allergic rhinoconjunctivitis and urticaria. Allergy.19 May 2010
[2]. María Luisa Lucero, et al. Preclinical toxicity profile of oral bilastine. Drug Chem Toxicol. 2012 Jun:35 Suppl 1:25-33. [Content Brief]
[3]. Roberta Verta, et al. Effect of Bilastine on Diabetic Nephropathy in DBA2/J Mice. Int J Mol Sci. 2019 May 24;20(10):2554. [Content Brief]
[4]. J Montoro, et al. Bilastine and the central nervous system. J Investig Allergol Clin Immunol. J Investig Allergol Clin Immuno [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1570 mL | 10.7849 mL | 21.5699 mL | 53.9246 mL |
| 5 mM | 0.4314 mL | 2.1570 mL | 4.3140 mL | 10.7849 mL | |
| 10 mM | 0.2157 mL | 1.0785 mL | 2.1570 mL | 5.3925 mL | |
| 15 mM | 0.1438 mL | 0.7190 mL | 1.4380 mL | 3.5950 mL | |
| 20 mM | 0.1078 mL | 0.5392 mL | 1.0785 mL | 2.6962 mL | |
| 25 mM | 0.0863 mL | 0.4314 mL | 0.8628 mL | 2.1570 mL |
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