Bepotastine free base

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

MedKoo CAT#: 314260

CAS#: 125602-71-3 (free base)

Description: Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. Bepotastine was approved in Japan for use in the treatment of allergic rhinitis and uriticaria/puritus in July 2000 and January 2002, respectively, and is marketed by Tanabe Seiyaku Co., Ltd. under the brand name Talion. It is available in oral and opthalmic dosage forms in Japan. The opthalmic solution is FDA approved since Sept 8, 2009 and is under the brand name Bepreve.

Chemical Structure

Bepotastine free base
CAS# 125602-71-3 (free base)

Theoretical Analysis

MedKoo Cat#: 314260
Name: Bepotastine free base
CAS#: 125602-71-3 (free base)
Chemical Formula: C21H25ClN2O3
Exact Mass: 388.15537
Molecular Weight: 388.8878
Elemental Analysis: C, 64.86; H, 6.48; Cl, 9.12; N, 7.20; O, 12.34

Price and Availability

Size Price Availability Quantity
100.0mg USD 450.0 2 weeks
200.0mg USD 650.0 2 weeks
500.0mg USD 1150.0 2 weeks
1.0g USD 1950.0 2 weeks
2.0g USD 2950.0 2 weeks
5.0g USD 4950.0 2 weeks
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Related CAS #: 125602-71-3 (free base)   190786-44-8 (besylate)   1160415-45-1 (tosylate)    

Synonym: TAU284; TAU-284; TAU 284; Bepotastine band name: Talion; Bepreve.

IUPAC/Chemical Name: 4-(4-((4-chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl)butanoic acid


InChi Code: InChI=1S/C21H25ClN2O3/c22-17-8-6-16(7-9-17)21(19-4-1-2-12-23-19)27-18-10-14-24(15-11-18)13-3-5-20(25)26/h1-2,4,6-9,12,18,21H,3,5,10-11,13-15H2,(H,25,26)


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: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 388.8878 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

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1: Lim DS, Youn YS, Kwack SJ, Kwak HM, Lim SK, Kim JY, Um YM, Lee JD, Hyeon JH, Kim YJ, Kim HS, Lee BM. Comparative efficacy and bioequivalence of novel h1-antihistamine bepotastine salts (nicotinate and salicylate). J Toxicol Environ Health A. 2014;77(22-24):1451-66. doi: 10.1080/15287394.2014.955833. PubMed PMID: 25343294.

2: Bergmann MT, Williams JI, Gomes PJ. Treatment of allergic conjunctivitis with bepotastine besilate ophthalmic solution 1.5%. Clin Ophthalmol. 2014 Aug 13;8:1495-505. doi: 10.2147/OPTH.S66637. eCollection 2014. PubMed PMID: 25152611; PubMed Central PMCID: PMC4140238.

3: Shentu J, Zhou H, Hu X, Wu G, Wu L, Zhu M, Zhai Y, Zheng Y, Liu J. Comparative fasting bioavailability of 2 bepotastine formulations in healthy male Chinese volunteers: an open-label, randomized, single-dose, 2-way crossover study. Clin Ther. 2014 Apr 1;36(4):579-85. doi: 10.1016/j.clinthera.2014.02.020. Epub 2014 Mar 18. PubMed PMID: 24656153.

4: Bielory L, Duttachoudhury S, McMunn A. Bepotastine besilate for the treatment of pruritus. Expert Opin Pharmacother. 2013 Dec;14(18):2553-69. doi: 10.1517/14656566.2013.849242. Epub 2013 Nov 5. Review. PubMed PMID: 24191914.

5: Kim KA, Park JY. Pharmacokinetic comparisons of bepotastine besilate and bepotastine salicylate in healthy subjects. Clin Drug Investig. 2013 Dec;33(12):913-9. doi: 10.1007/s40261-013-0140-7. PubMed PMID: 24105252.

6: Choi YK, Chung YH, Nam YS, Kang da Y, Kim H, Lee SE, Kim HR, Lee YS, Jeong JH. UPLC-MS/MS method for determination of bepotastine in human plasma. J Chromatogr Sci. 2014 Sep;52(8):886-93. doi: 10.1093/chromsci/bmt135. Epub 2013 Sep 10. PubMed PMID: 24023058.

7: Carr WW, Nayak AS, Ratner PH, Gow JA, McNamara TR, Williams JI; Bepotastine Besilate Ophthalmic Solution 1.5% (Bepreve) Study Group. Efficacy of bepotastine besilate ophthalmic solution 1.5% for seasonal allergic conjunctivitis: a randomized, placebo-controlled, natural exposure, clinical trial. Allergy Asthma Proc. 2013 May-Jun;34(3):247-54. PubMed PMID: 23484763.

8: McCabe CF, McCabe SE. Comparative efficacy of bepotastine besilate 1.5% ophthalmic solution versus olopatadine hydrochloride 0.2% ophthalmic solution evaluated by patient preference. Clin Ophthalmol. 2012;6:1731-8. doi: 10.2147/OPTH.S35431. Epub 2012 Oct 29. PubMed PMID: 23152650; PubMed Central PMCID: PMC3497448.

9: Meier EJ, Torkildsen GL, Gow JA, McNamara TR, Gomes PJ, Williams JI; Bepotastine Besilate Ophthalmic Solutions Study Group. Integrated phase III trials of bepotastine besilate ophthalmic solution 1.5% for ocular itching associated with allergic conjunctivitis. Allergy Asthma Proc. 2012 May-Jun;33(3):265-74. PubMed PMID: 22991696.

10: Cho KH, Choi HG. Development of novel bepotastine salicylate salt bioequivalent to the commercial bepotastine besilate in beagle dogs. Drug Dev Ind Pharm. 2013 Jun;39(6):901-8. doi: 10.3109/03639045.2012.717295. Epub 2012 Sep 10. PubMed PMID: 22963365.