Ebastine
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MedKoo CAT#: 317143

CAS#: 90729-43-4

Description: Ebastine, is a H1 antihistamine with low potential for causing drowsiness. It does not penetrate the blood–brain barrier to a significant amount and thus combines an effective block of the H1 receptor in peripheral tissue with a low incidence of central side effects, i.e. seldom causing sedation or drowsiness. After oral administration, ebastine undergoes extensive first-pass metabolism by hepatic cytochrome P450 3A4 into its active carboxylic acid metabolite, carebastine. This conversion is practically complete. Ebastine is a second-generation H1 receptor antagonist that is indicated mainly for allergic rhinitis and chronic idiopathic urticaria.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 90 2 weeks
25mg USD 150 2 weeks
50mg USD 250 2 weeks
100mg USD 350 2 weeks
200mg USD 450 2 weeks
500mg USD 550 2 weeks
1g USD 650 2 weeks
2g USD 950 2 weeks
5g USD 1650 2 weeks
10g USD 2650 2 weeks
20g USD 3650 2 weeks
50g USD 5950 2 weeks
Inquire bulk and customized quantity

Pricing updated 2020-08-08. Prices are subject to change without notice.

Ebastine, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 317143
Name: Ebastine
CAS#: 90729-43-4
Chemical Formula: C32H39NO2
Exact Mass: 469.29808
Molecular Weight: 469.67
Elemental Analysis: C, 81.83; H, 8.37; N, 2.98; O, 6.81


Synonym: RP64305; RP-64305; RP 64305; LAS W-090; Ebastine; Brand name: Evastin; Kestine; Ebastel; Aleva; Ebatrol; Bactil; Busidril; Ebastel; Evastel; Kestin; Kestine.

IUPAC/Chemical Name: 4-(4-(benzhydryloxy)piperidin-1-yl)-1-(4-(tert-butyl)phenyl)butan-1-one

InChi Key: MJJALKDDGIKVBE-UHFFFAOYSA-N

InChi Code: InChI=1S/C32H39NO2/c1-32(2,3)28-18-16-25(17-19-28)30(34)15-10-22-33-23-20-29(21-24-33)35-31(26-11-6-4-7-12-26)27-13-8-5-9-14-27/h4-9,11-14,16-19,29,31H,10,15,20-24H2,1-3H3

SMILES Code: O=C(CCCN1CCC(OC(C2=CC=CC=C2)C3=CC=CC=C3)CC1)C4=CC=C(C(C)(C)C)C=C4


Technical Data

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, not in water

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:
2934.99.9001


References

1: Jung HS, Park CH, Park YT, Bae MA, Lee YI, Kang BJ, Jegal Y, Ahn JJ, Lee T. Gynecomastia induced by H1-antihistamine (ebastine) in a patient with idiopathic anaphylaxis. Asia Pac Allergy. 2015 Jul;5(3):187-90. doi: 10.5415/apallergy.2015.5.3.187. Epub 2015 Jul 29. PubMed PMID: 26240797; PubMed Central PMCID: PMC4521169.

2: Rapolu R, Pandey AK, Raju ChK, Ghosh K, Srinivas K, Awasthi A, Navalgund SG, Surendranath KV. A novel UV degradation product of Ebastine: isolation and characterization using Q-TOF, NMR, IR and computational chemistry. J Pharm Biomed Anal. 2015 Mar 25;107:488-94. doi: 10.1016/j.jpba.2015.01.039. Epub 2015 Jan 29. PubMed PMID: 25679093.

3: Ibrahim FA, Wahba ME. Orthogonal projection to latent structures combined with artificial neural networks in non-destructive analysis of ebastine powder. Acta Chim Slov. 2014;61(1):11-8. PubMed PMID: 24664321.

4: Rana NS, Rajesh KS, Patel NN, Patel PR, Limbachiya U, Pasha TY. Development and Validation of RP-HPLC Method for the Simultaneous Estimation of Montelukast Sodium and Ebastine in Tablet Dosage Form. Indian J Pharm Sci. 2013 Sep;75(5):599-602. PubMed PMID: 24403662; PubMed Central PMCID: PMC3877523.

5: Schmidt AH, Molnár I. Using an innovative Quality-by-Design approach for development of a stability indicating UHPLC method for ebastine in the API and pharmaceutical formulations. J Pharm Biomed Anal. 2013 May 5;78-79:65-74. doi: 10.1016/j.jpba.2013.01.032. Epub 2013 Jan 31. PubMed PMID: 23454599.

6: Haggag RS, Belal TS. Gradient HPLC-DAD determination of two pharmaceutical mixtures containing the antihistaminic drug ebastine. J Chromatogr Sci. 2012 Nov-Dec;50(10):862-8. doi: 10.1093/chromsci/bms082. Epub 2012 Jun 7. PubMed PMID: 22677488.

7: Godse KV. Ebastine in chronic spontaneous urticaria in higher doses. Indian J Dermatol. 2011 Sep-Oct;56(5):597-8. doi: 10.4103/0019-5154.87168. PubMed PMID: 22121291; PubMed Central PMCID: PMC3221236.

8: Ibrahim F, Sharaf El-Din MK, Eid MI, Wahba ME. Validated stability indicating liquid chromatographic determination of ebastine in pharmaceuticals after pre column derivatization: Application to tablets and content uniformity testing. Chem Cent J. 2011 May 9;5:24. doi: 10.1186/1752-153X-5-24. PubMed PMID: 21554731; PubMed Central PMCID: PMC3113337.

9: Kang W, Elitzer S, Noh K, Bednarek T, Weiss M. Myocardial pharmacokinetics of ebastine, a substrate for cytochrome P450 2J, in rat isolated heart. Br J Pharmacol. 2011 Aug;163(8):1733-9. doi: 10.1111/j.1476-5381.2011.01338.x. PubMed PMID: 21410688; PubMed Central PMCID: PMC3166699.

10: Ibrahim F, El-Din MK, Eid MI, Wahba ME. Validated stability-indicating spectrofluorimetric methods for the determination of ebastine in pharmaceutical preparations. Chem Cent J. 2011 Mar 8;5(1):11. doi: 10.1186/1752-153X-5-11. PubMed PMID: 21385439; PubMed Central PMCID: PMC3061886.

11: Ciprandi G. Clinical utility and patient adherence with ebastine for allergic rhinitis. Patient Prefer Adherence. 2010 Oct 14;4:389-95. doi: 10.2147/PPA.S8186. PubMed PMID: 21206514; PubMed Central PMCID: PMC3003605.

12: Ohyama M, Shimizu A, Tanaka K, Amagai M. Experimental evaluation of ebastine, a second-generation anti-histamine, as a supportive medication for alopecia areata. J Dermatol Sci. 2010 May;58(2):154-7. doi: 10.1016/j.jdermsci.2010.03.009. Epub 2010 Mar 23. PubMed PMID: 20388588.

13: Shon JH, Yeo CW, Liu KH, Lee SS, Cha IJ, Shin JG. Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants. J Clin Pharmacol. 2010 Feb;50(2):195-204. doi: 10.1177/0091270009348974. Epub 2009 Oct 19. PubMed PMID: 19841159.

14: Aguilar D, Arias A, Báez C, González S, Hernández D, Linares FJ, López A, Macías A, Martínez A, Martínez HM, Martínez N, Mogica MD, Paz D, Rojo I, Sánchez A. [Multicenter study of satisfaction with fast-dissolving ebastine, 20 mg/ day, in Mexican patients with allergic rhinitis]. Rev Alerg Mex. 2009 Mar-Apr;56(2):36-40. Spanish. PubMed PMID: 19526952.

15: Magerl M, Schmolke J, Metz M, Zuberbier T, Siebenhaar F, Maurer M. Prevention of signs and symptoms of dermographic urticaria by single-dose ebastine 20 mg. Clin Exp Dermatol. 2009 Jul;34(5):e137-40. doi: 10.1111/j.1365-2230.2008.03097.x. Epub 2009 Mar 23. PubMed PMID: 19323664.

16: Ciprandi G, Cirillo I, Pistorio A, Di Gioacchino M, Fenoglio D. Ebastine increases IFN-gamma production in patients with persistent allergic rhinitis. J Biol Regul Homeost Agents. 2009 Jan-Mar;23(1):31-6. PubMed PMID: 19321044.

17: Tsiskarishvili NV, Dundua MM, Tsiskarishvili NI. [Avene-50 and Ebastine in treatment and prevention of photodermatosis]. Georgian Med News. 2009 Feb;(167):52-6. Russian. PubMed PMID: 19276471.

18: Rico S, Antonijoan R, Barbanoj M. Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines. J Asthma Allergy. 2009 Aug 31;2:73-92. PubMed PMID: 21437146; PubMed Central PMCID: PMC3048600.

19: Sastre J. Ebastine in allergic rhinitis and chronic idiopathic urticaria. Allergy. 2008 Dec;63 Suppl 89:1-20. doi: 10.1111/j.1398-9995.2008.01897.x. Review. PubMed PMID: 19032340.

20: Roger A, Fortea J, Mora S, Artés M. Patient assessment of onset of action and overall satisfaction with ebastine fast-dissolving tablets in allergic rhinitis. Expert Rev Pharmacoecon Outcomes Res. 2008 Aug;8(4):337-42. doi: 10.1586/14737167.8.4.337. PubMed PMID: 20528340.