Name: Bilastine
Brand: Selleck Chemicals
SKU: S3721
Rating: 5 (1 reviews)

Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.

Bilastine Chemical Structure

CAS: 202189-78-4

Purity & Quality Control

Batch: S372101 4-Methylpyridine] 29 mg/mL] false] DMSO] 1 mg/mL] false] Water] Insoluble] false Purity: 99.87%

99.87

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Signaling Pathway

Histamine Receptor Signaling Pathway

Choose Selective Histamine Receptor Inhibitors

Biological Activity

Description

Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.

Targets

H1 receptor ^[2]
(in guinea-pig cerebellum)

44.15 nM(Ki)

In vitro
In vitro	Bilastine has a high specific affinity for the H1-receptor but it has no or very low affinity for 30 other tested receptors^[1]. It is lack of significant antagonism against serotonin, bradykinin, leukotriene D4, calcium, muscarinic M3-receptors, α1-adrenoceptors, β2-adrenoceptors, and H2- and H3- receptors^[2].

In Vivo
In vivo	Bilastine is efficacious in all nasal symptoms including obstruction and in eye symptoms in patients with allergic rhinoconjunctivitis. Bilastine is well tolerated. In the fasting state bilastine is quickly absorbed, but the absorption is slowed when it is taken with food or fruit juice. In vivo studies in rats have demonstrated reduction in histamine-stimulated smooth muscular contraction, bronchospasms, endothelial permeability, and microvascular extravasation^[1].

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT02213367	Completed	Chronic Urticaria	Charite University Berlin Germany	July 2014	Phase 3
NCT01271075	Completed	Cold Contact Urticaria	Charite University Berlin Germany\|Faes Farma S.A.	September 2010	Phase 2\|Phase 3
NCT01124123	Completed	Healthy	Faes Farma S.A.	May 2010	Phase 1
NCT01081574	Completed	Allergic Rhinoconjunctivitis\|Chronic Urticaria	Faes Farma S.A.	January 2010	Phase 1\|Phase 2

References

Chemical Information & Solubility

Molecular Weight	463.61	Formula	C₂₈H₃₇N₃O₃
CAS No.	202189-78-4	SDF	Download Bilastine SDF
Smiles	CCOCCN1C2=CC=CC=C2N=C1C3CCN(CC3)CCC4=CC=C(C=C4)C(C)(C)C(=O)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

4-Methylpyridine : 29 mg/mL

DMSO : 1 mg/mL ( (2.15 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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