Bilastine | CAS#202189-78-4 | antihistamine

Bilastine
new

featured

WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 314243

CAS#: 202189-78-4

Description: Bilastine (trade name Bilaxten) is a second generation antihistamine drug for the treatment of allergic rhinoconjunctivitis and urticaria (hives). It exerts its effect as a selective histamine H1 receptor antagonist, and has a potency similar to cetirizine and is superior to fexofenadine. It was developed in Spain by FAES Farma. Bilastine is approved in the European Union for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria, but it is not approved by the U.S. Food and Drug Administration for any use in the United States. Bilastine has been effective in the treatment of ocular symptoms and diseases of allergies, including rhinoconjuctivitis. Additionally, bilastine has been shown to improve quality of life, and all nasal and ocular symptoms related to allergic rhinitis.

Chemical Structure

Bilastine

CAS# 202189-78-4

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 314243
Name: Bilastine
CAS#: 202189-78-4
Chemical Formula: C28H37N3O3
Exact Mass: 463.28
Molecular Weight: 463.610
Elemental Analysis: C, 72.54; H, 8.04; N, 9.06; O, 10.35

Price and Availability

Size	Price	Availability
25mg	USD 90	Ready to ship
50mg	USD 150	Ready to ship
100mg	USD 250	Ready to ship
200mg	USD 450	Ready to ship
500mg	USD 950	Ready to ship
1g	USD 1650	Ready to ship
2g	USD 2950	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Bilastine trade name Bilaxten

IUPAC/Chemical Name: 2-(4-(2-(4-(1-(2-ethoxyethyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic acid

InChi Key: ACCMWZWAEFYUGZ-UHFFFAOYSA-N

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)

SMILES Code: CC(C)(C1=CC=C(CCN2CCC(C3=NC4=CC=CC=C4N3CCOCC)CC2)C=C1)C(O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO.

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2933998090

More Info:

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#C9R10B23

QC Data:

View QC data: current batch, Lot#C9R10B23

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	Bilastine is a selective histamine H1 receptor antagonist.
In vitro activity:	TBD
In vivo activity:	Interestingly, an apparent discrepancy between functional and morphological data appears. Indeed, while only bilastine 30 mg/kg showed a full protection of renal function, matrix mesangial expansion and collagen deposition were significantly affected by bilastine, irrespective of the dose. However, these are both pro-fibrotic events that could be related to the general anti-inflammatory effect of bilastine, also confirmed in this study in terms of reduction of infiltrating cells. On the contrary, the biochemical evaluation (nephrin, synaptopodin, and P-cadherin expression), keeping with the functional analysis, reached statistical significance only by bilastine at 30 mg/kg. Therefore, histamine could be a trigger stimulus for the renal inflammatory response induced by hyperglycaemia, but is also a contributor to the podocyte junctional integrity, to which other mediators, such as angiotensin II, participate as well. The observed effect of bilastine is possibly due to the haemodynamic regulation induced by blocking H1 receptor. Reference: Int J Mol Sci. 2019 May; 20(10): 2554. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6566437/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	49.3	106.34

Preparing Stock Solutions

The following data is based on the product molecular weight 463.61 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Verta R, Grange C, Gurrieri M, Borga S, Nardini P, Argenziano M, Ghè C, Cavalli R, Benetti E, Miglio G, Bussolati B, Pini A, Rosa AC. Effect of Bilastine on Diabetic Nephropathy in DBA2/J Mice. Int J Mol Sci. 2019 May 24;20(10):2554. doi: 10.3390/ijms20102554. PMID: 31137660; PMCID: PMC6566437. 2. Corcóstegui R, Labeaga L, Innerárity A, Berisa A, Orjales A. In vivo pharmacological characterisation of bilastine, a potent and selective histamine H1 receptor antagonist. Drugs R D. 2006;7(4):219-31. doi: 10.2165/00126839-200607040-00002. PMID: 16784247.
In vitro protocol:	TBD
In vivo protocol:	1. Verta R, Grange C, Gurrieri M, Borga S, Nardini P, Argenziano M, Ghè C, Cavalli R, Benetti E, Miglio G, Bussolati B, Pini A, Rosa AC. Effect of Bilastine on Diabetic Nephropathy in DBA2/J Mice. Int J Mol Sci. 2019 May 24;20(10):2554. doi: 10.3390/ijms20102554. PMID: 31137660; PMCID: PMC6566437. 2. Corcóstegui R, Labeaga L, Innerárity A, Berisa A, Orjales A. In vivo pharmacological characterisation of bilastine, a potent and selective histamine H1 receptor antagonist. Drugs R D. 2006;7(4):219-31. doi: 10.2165/00126839-200607040-00002. PMID: 16784247.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

1: Church MK, Tiongco-Recto M, Ridolo E, Novák Z. Bilastine: a lifetime companion for the treatment of allergies. Curr Med Res Opin. 2020 Mar;36(3):445-454. doi: 10.1080/03007995.2019.1681134. Epub 2019 Nov 13. PMID: 31612732.

2: Singh Randhawa A, Mohd Noor N, Md Daud MK, Abdullah B. Efficacy and Safety of Bilastine in the Treatment of Allergic Rhinitis: A Systematic Review and Meta- analysis. Front Pharmacol. 2022 Jan 10;12:731201. doi: 10.3389/fphar.2021.731201. PMID: 35082662; PMCID: PMC8784885.

3: Rodríguez Del Río P, Rodríguez Fernández F, Ballester Asensio E, Tortajada- Girbés M. How bilastine is used to treat allergic rhinitis and urticaria in children. Immunotherapy. 2022 Jan;14(1):77-89. doi: 10.2217/imt-2021-0251. Epub 2021 Dec 1. PMID: 34850647.

4: Bilastine for allergic rhinoconjunctivitis, urticaria. Aust Prescr. 2022 Oct;45(5):179. doi: 10.18773/austprescr.2022.057. Epub 2022 Sep 1. PMID: 36382168; PMCID: PMC9584787.

5: Wang XY, Lim-Jurado M, Prepageran N, Tantilipikorn P, Wang de Y. Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine. Ther Clin Risk Manag. 2016 Apr 13;12:585-97. doi: 10.2147/TCRM.S105189. PMID: 27110120; PMCID: PMC4835134.

6: Abdelshafy AM, Abdallah SY, Hassan AF, Mohamed HA, Kamal NM, Ali ST, Abdelhaleem IA. The Impact of Bilastine on Symptoms of Allergic Rhinitis and Chronic Urticaria: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Am J Rhinol Allergy. 2022 Sep;36(5):684-694. doi: 10.1177/19458924221097449. Epub 2022 May 20. PMID: 35593100.

7: Leceta A, García A, Sologuren A, Campo C. Bilastine 10 and 20 mg in paediatric and adult patients: an updated practical approach to treatment decisions. Drugs Context. 2021 Aug 10;10:2021-5-1. doi: 10.7573/dic.2021-5-1. PMID: 34457015; PMCID: PMC8366504.

8: Jáuregui I, Ferrer M, Bartra J, del Cuvillo A, Dávila I, Montoro J, Mullol J, Sastre J, Valero A. Bilastine for the treatment of urticaria. Expert Opin Pharmacother. 2013 Aug;14(11):1537-44. doi: 10.1517/14656566.2013.800044. Epub 2013 May 16. PMID: 23675825.

9: Church MK, Labeaga L. Bilastine: a new H1 -antihistamine with an optimal profile for updosing in urticaria. J Eur Acad Dermatol Venereol. 2017 Sep;31(9):1447-1452. doi: 10.1111/jdv.14305. Epub 2017 Jun 1. PMID: 28467671.

10: Jáuregui I, Ramaekers JG, Yanai K, Farré M, Redondo E, Valiente R, Labeaga L. Bilastine: a new antihistamine with an optimal benefit-to-risk ratio for safety during driving. Expert Opin Drug Saf. 2016 Jan;15(1):89-98. doi: 10.1517/14740338.2016.1112786. Epub 2015 Nov 16. PMID: 26571227.

11: Podder I, Das A, Ghosh S, Biswas D, Sengupta S, Chowdhury SN. Effectiveness, safety, and tolerability of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic spontaneous urticaria: A double-blind, parallel group, randomized controlled trial. Dermatol Ther. 2020 Nov;33(6):e13946. doi: 10.1111/dth.13946. Epub 2020 Jul 27. PMID: 32618048.

12: Sádaba Díaz de Rada B, Azanza Perea JR, Gomez-Guiu Hormigos A. Bilastine for the relief of allergy symptoms. Drugs Today (Barc). 2011 Apr;47(4):251-62. doi: 10.1358/dot.2011.47.4.1587029. PMID: 21573249.

13: Carter NJ. Bilastine: in allergic rhinitis and urticaria. Drugs. 2012 Jun 18;72(9):1257-69. doi: 10.2165/11209310-000000000-00000. PMID: 22686617.

14: Leceta A, Sologuren A, Valiente R, Campo C, Labeaga L. Bilastine in allergic rhinoconjunctivitis and urticaria: a practical approach to treatment decisions based on queries received by the medical information department. Drugs Context. 2017 Feb 3;6:212500. doi: 10.7573/dic.212500. PMID: 28210286; PMCID: PMC5299972.

15: Jáuregui I, Bartra J, del Cuvillo A, Dávila I, Ferrer M, Montoro J, Mullol J, Sastre J, Valero A. Bilastine and quality of life. J Investig Allergol Clin Immunol. 2011;21 Suppl 3:16-23. PMID: 22185046.

16: Lynde CW, Sussman G, Dion PL, Guenther L, Hébert J, Rao J, Leek TV, Waserman S. Multidisciplinary Real-World Experience With Bilastine, a Second Generation Antihistamine. J Drugs Dermatol. 2020 Feb 1;19(2):145-154. doi: 10.36849/JDD.2020.4835. PMID: 32129958.

17: Scaglione F. Safety profile of bilastine: 2nd generation H1-antihistamines. Eur Rev Med Pharmacol Sci. 2012 Dec;16(14):1999-2005. PMID: 23242729.

18: Shah B, Dhoot D, Choudhary A, Jangid N, Mistry D, Shah S, Kamat S, Barkate H. A Comparative, Three-Arm, Randomized Clinical Trial to Evaluate the Effectiveness and Tolerability of Bilastine vs Fexofenadine vs Levocetirizine at the Standard Dose and Bilastine vs Fexofenadine at Higher Than the Standard Dose (Up-Dosing) vs Levocetirizine and Hydroxyzine (in Combination) in Patients with Chronic Spontaneous Urticaria. Clin Cosmet Investig Dermatol. 2022 Feb 18;15:261-270. doi: 10.2147/CCID.S350122. PMID: 35221703; PMCID: PMC8867222.

19: Lucero ML, Peither A, Ledo F. Bilastine: an environmental risk assessment. Drug Chem Toxicol. 2015 Oct;38(4):460-8. doi: 10.3109/01480545.2014.992438. Epub 2015 Jan 22. PMID: 25609003.

20: Montoro J, Mullol J, Dávila I, Ferrer M, Sastre J, Bartra J, Jáuregui I, del Cuvillo A, Valero A. Bilastine and the central nervous system. J Investig Allergol Clin Immunol. 2011;21 Suppl 3:9-15. PMID: 22185045.

Your view history

Bilastine new featured