BILASTINE
Bilastine is a research-grade compound used in advanced pharmaceutical and biochemical studies. Chemical & Pharmacological Characteristics Bilastine is a polar, drug-like small molecule with high affinity for the histamine H1 receptor and limited penetration into the central nervous system under typical conditions. In vitro performance depends on receptor expression, assay buffer composition, and potential transporter effects. Formulation and solubility control are important for consistent exposure in cell-based assays. It is primarily applied to investigate compound-specific mechanisms, physicochemical behavior, and analytical or formulation-relevant characteristics under controlled
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Product Description
Chemical & Pharmacological Characteristics
Bilastine is a polar, drug-like small molecule with high affinity for the histamine H1 receptor and limited penetration into the central nervous system under typical conditions. In vitro performance depends on receptor expression, assay buffer composition, and potential transporter effects. Formulation and solubility control are important for consistent exposure in cell-based assays.
Mechanism of Action
Bilastine acts as a competitive antagonist at the H1 receptor, reducing histamine-driven signaling that promotes vasodilation, increased vascular permeability, pruritus, and sensory neuron activation.
By stabilizing the inactive receptor state, it attenuates downstream G-protein mediated pathways, reducing inflammatory mediator amplification and symptom-linked signaling. Mechanistic studies should distinguish direct H1 blockade from secondary reductions in cytokine and neurogenic inflammation markers.
Advanced Research Applications
- H1 receptor pharmacology and antagonist potency benchmarking
- Allergy and urticaria pathway modeling with histamine challenge systems
- Mast cell mediator and neurogenic itch signaling studies
- Comparative profiling versus sedating antihistamines in CNS liability panels
- Exposure-response and transporter impact evaluation in epithelial models
Toxicodynamics & Cellular Hazard Spectrum
- Low CNS sedation expected, but high exposure can still alter neuronal readouts
- Potential assay artifacts from transporter interactions and protein binding
- Off-target effects at supraphysiologic concentration; confirm selectivity controls
- Solubility limits can drive aggregation and non-linear exposure; verify dosing
- Use standard PPE and avoid unintended biological exposure
For expert laboratory research only – not intended for biological or therapeutic exposure.
Datasheet
| Molecular Formula | C28H37N3O3 |
|---|---|
| Molecular Weight | 463.6 g/mol |
| CAS Number | 202189-78-4 |
| Storage Condition | Store in a cool, dry place. Keep container tightly closed. Protect from moisture and light. |
| Solubility | Solubility depends on solvent and conditions (e.g., pH). Please contact us for solvent-specific guidance. |
| Purity | Purity information is available upon request (COA). |
| Synonym | Bilastine; 202189-78-4; Ilaxten; 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid; Bilastina |
| IUPAC/Chemical Name | 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid |
| InChl Key | ACCMWZWAEFYUGZ-UHFFFAOYSA-N |
| InChl 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) |
| References | https://pubchem.ncbi.nlm.nih.gov/compound/185460; small-molecule |
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