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

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

10mg
USD 90
100mg
USD 350
1g
USD 650
10g
USD 2650
100g
Ask price
Size
Price

25mg
USD 150
200mg
USD 450
2g
USD 950
20g
USD 3650
Size
Price

50mg
USD 250
500mg
USD 550
5g
USD 1650
50g
USD 5950

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).

Harmonized System Code:
293490


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.