Bilastine

SKU: orb1303023

Description

Bilastine is a potent and selective second-generation H1 receptor antagonist, characterized by its fast onset and long-lasting activity. It is widely used in pharmacological research for studying allergic responses and histamine signaling in both in vitro binding assays and in vivo models of allergy and inflammation.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 202189-78-4
• MW: 463.61
• Purity: >99.99% (May vary between batches)
• Formula: C₂₈H₃₇N₃O₃
• SMILES: CCOCCn1c(nc2ccccc12)C1CCN(CCc2ccc(cc2)C(C)(C)C(O)=O)CC1
• Target: Histamine Receptor
• Solubility: DMSO:Slightly soluble

Bioactivity

• Target IC50:
  H1 receptor(guinea-pig cerebellum):44.15 nM(Ki)
• In Vivo:
  In patients with allergic rhinoconjunctivitis, Bilastine is efficacious in all nasal symptoms including obstruction and in eye symptoms. In the fasting state, Bilastine is quickly absorbed, but the absorption is slowed when it is taken with food or fruit juice.
• In Vitro:
  Bilastine has a highly selective affinity for the H1-receptor but a very low affinity for 30 other tested receptors. It isn't obvious inhibitory against bradykinin, serotonin, muscarinic M3-receptors, leukotriene D4, calcium, α1-adrenoceptors, β2-adrenoceptors, and H2- and H3- receptors.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bilastine, Bilaxten, inhibit, Inhibitor, HistamineReceptor, Histamine Receptor, H1 receptor

Compound Identifiers

PubChem CID

185460