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MedKoo Cat#: 314243 | Name: Bilastine
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Description:

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

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
Bilastine
CAS#202189-78-4

Theoretical Analysis

MedKoo Cat#: 314243

Name: Bilastine

CAS#: 202189-78-4

Chemical Formula: C28H37N3O3

Exact Mass: 463.2835

Molecular Weight: 463.61

Elemental Analysis: C, 72.54; H, 8.04; N, 9.06; O, 10.35

Price and Availability

Size Price Availability Quantity
25mg USD 90.00 Ready to ship
50mg USD 150.00 Ready to ship
100mg USD 250.00 Ready to ship
200mg USD 450.00 Ready to ship
500mg USD 950.00 Ready to ship
1g USD 1,650.00 Ready to ship
2g USD 2,950.00 Ready to ship
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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
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/
Solvent mg/mL mM
Solubility
DMSO 49.3 106.34
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

Recalculate based on batch purity %
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.
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.