| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Animal Protocol |
Tissue Collection for Ex Vivo Experiments:** The study describes numerous protocols for obtaining tissues from animals for ex vivo pharmacological experiments. These include:
* Guinea pigs (male, 400-600g) for cerebellum (H₁ binding), ileum (H₁ antagonism, bradykinin antagonism, calcium antagonism, M₃ antagonism, Schultz-Dale reaction), trachea (H₁ antagonism, LTD₄ antagonism, β₂-adrenoceptor antagonism), right atria (H₂ antagonism), and jejunum (H₃ antagonism). Animals were typically killed by decapitation or cervical dislocation [1]. * Rats (Wistar, 250-300g) for caudal artery (5-HT₂A antagonism). Animals were sacrificed by asphyxia in a CO₂ atmosphere and exsanguinated [1]. * Rabbits (New Zealand, 2-2.5 kg) for thoracic aorta (α₁-adrenoceptor antagonism). Animals were anesthetized and exsanguinated prior to tissue removal [1]. |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The time to peak concentration (Tmax) of Bilastine is 1.13 hours. The absolute bioavailability is 61%. No drug accumulation was observed after 14 days of daily administration of 20-100 mg. Compared to fasting, peak plasma concentration (Cmax) decreased by 25% and 33% when co-administered with a low-fat meal and a high-fat meal, respectively. Co-administration with grapefruit juice reduced Cmax by 30%. Bilastine is primarily excreted in feces (66.5%), with a small amount excreted in urine (28.3%). Almost all of it is excreted unchanged. The total clearance of Bilastine is 9.20 L/h, and the renal clearance is 8.7 L/h. Metabolism/Metabolites Bilastine does not interact with the cytochrome P450 system and is not significantly metabolized in humans. Biological half-life The average elimination half-life is 14.5 hours. |
| Toxicity/Toxicokinetics |
Protein Binding
Bilastine binds to human plasma proteins at a rate of 84-90%. |
| References |
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| Additional Infomation |
Bilastine belongs to the benzimidazole class of drugs. Bilastine is a novel, next-generation antihistamine with high selectivity for H1 histamine receptors, exhibiting rapid onset and long duration of action. Indications: For the relief of nasal and non-nasal symptoms of seasonal rhinitis in patients aged 12 years and older, and for the relief of symptoms of chronic spontaneous urticaria in patients aged 18 years and older. FDA Label: Treatment of allergic conjunctivitis, treatment of acute type I hypersensitivity reactions, treatment of allergic rhinoconjunctivitis, treatment of urticaria, treatment of urticaria, treatment of allergic rhinoconjunctivitis. Mechanism of Action: Bilastine is a selective histamine H1 receptor antagonist (Ki = 64 nM). During an allergic reaction, mast cells degranulate, releasing histamine and other substances. Bilastine reduces allergic symptoms caused by histamine release from mast cells by binding to H1 receptors and preventing their activation.
Pharmacodynamics Bilastine is an antihistamine that can relieve allergy symptoms such as nasal congestion and hives. |
| Molecular Formula |
C28H37N3O3
|
|---|---|
| Molecular Weight |
463.6117
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| Exact Mass |
463.283
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| Elemental Analysis |
C, 72.54; H, 8.04; N, 9.06; O, 10.35
|
| CAS # |
202189-78-4
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| Related CAS # |
Bilastine-d6;1215358-58-9
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| PubChem CID |
185460
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
639.1±55.0 °C at 760 mmHg
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| Melting Point |
202 °C
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| Flash Point |
340.3±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
|
| Index of Refraction |
1.594
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| LogP |
5.06
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
34
|
| Complexity |
641
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])N1C2=C([H])C([H])=C([H])C([H])=C2N=C1C1([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])C2C([H])=C([H])C(=C([H])C=2[H])C(C(=O)O[H])(C([H])([H])[H])C([H])([H])[H])C([H])([H])C1([H])[H]
|
| InChi Key |
ACCMWZWAEFYUGZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H37N3O3/c1-4-34-20-19-31-25-8-6-5-7-24(25)29-26(31)22-14-17-30(18-15-22)16-13-21-9-11-23(12-10-21)28(2,3)27(32)33/h5-12,22H,4,13-20H2,1-3H3,(H,32,33)
|
| Chemical Name |
2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid
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| Synonyms |
Bilastine trade name Bilaxten
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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 |
| 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) |
DMSO : ~10 mg/mL (~21.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (4.31 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 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 mg/mL (4.31 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 20.0 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. View More
Solubility in Formulation 3: ≥ 2 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1570 mL | 10.7849 mL | 21.5699 mL | |
| 5 mM | 0.4314 mL | 2.1570 mL | 4.3140 mL | |
| 10 mM | 0.2157 mL | 1.0785 mL | 2.1570 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.
Quality of Life in Patients With Allergic Rhinitis: Clinical Trial With Bilastine or Loratadine
CTID: NCT02513290
Phase: Phase 4 Status: Completed
Date: 2018-05-07
Products are for research use only; We do not sell to patients
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