Bepotastine Besilate (Bepreve)

Alias: TAU 284; Bepotastine besylate; bepotastine besilate; TAU-284; TAU284;Bepreve; Talion
Cat No.:V1212 Purity: ≥98%
Bepotastinebesilate(bepotastine besylate; TAU-284; TAU284;Bepreve; Talion), the besylate salt ofBepotastine, is a 2nd generation, non-sedating, and selective antagonist of histamine 1 (H1) receptor with a pIC50 of 5.7.
Bepotastine Besilate (Bepreve) Chemical Structure CAS No.: 190786-44-8
Product category: Histamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of Bepotastine Besilate (Bepreve):

  • (Rac)-Bepotastine besilate
  • Bepotastine
  • Bepotastine Tosylate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Bepotastine besilate (bepotastine besylate; TAU-284; TAU284; Bepreve; Talion), the besylate salt of Bepotastine, is a 2nd generation, non-sedating, and selective antagonist of histamine 1 (H1) receptor with a pIC50 of 5.7. Bepostatine besilate has been given approval to treat pruritus, urticaria, and allergic rhinitis. By blocking histamine H1 receptors, antagonistically opposing the vasoconstrictor and, to a lesser degree, the vasodilator effects of histamine, bepotastine besilate inhibits the action of histamine. Mast cell stabilisers work by stopping the regular flow of intracellular signals, which inhibits degranulation and the subsequent release of histamine. Talion is the brand name for bepostatine besilate.

Biological Activity I Assay Protocols (From Reference)
Targets
Histamine H1 receptor ( pIC50 = 5.7 )
ln Vitro

In vitro activity: Bepotastine besilate (10, 100, 1000 µM; preincubates for 120 min) reaches a statistically significant reduction in the amount of histamine released as a result of treatment with A23187 at 1000 µM[1].
Bepotastine besilate (50 µM; 1 h) inhibits NGF mRNA expression in NHEKs[2].

ln Vivo
Bepotastine besilate (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) significantly inhibits the infiltration of conjunctival eosinophils induced by PAF[1].
Bepotastine besilate (3 mg/kg; p.o.; once) suppresses scratching behavior to a frequency of 59.0 and a duration of 14.57 seconds, near identical levels to the control[3].
Bepotastine besilate (10 mg/kg; p.o.; once) (10 mg/kg; p.o.; once) considerably reduces serum LTB 4 levels to 711.3 pg/mL at 1 h and 858.8 pg/mL at 2 h in NC/Nga mice with a rash[3].
Cell Assay
Cell Line: NHEKs
Concentration: 50 µM (preincubation)
Incubation Time: 1 h
Result: Suppressed the expression of NGF mRNA in NHEKs.
Animal Protocol
Guinea pigs (6-week-old)
10 g/L (1.0% (w/v)) for 10 µL
Eye drop; 3 times at intervals of 20 min (in one eye).
References

[1]. Bepotastine besilate, a highly selective histamine H(1) receptor antagonist, suppresses vascular hyperpermeability and eosinophil recruitment in in vitro and in vivo experimental allergic conjunctivitis models. Exp Eye Res. 2010 Jul;91(1):8.

[2]. Bepotastine besilate downregulates the expression of nerve elongation factors in normal human epidermal keratinocytes. J Dermatol Sci. 2018 Apr 23:S0923-1811(18)30186-5.

[3]. Oral administration of bepotastine besilate suppressed scratching behavior of atopic dermatitis model NC/Nga mice. Int Arch Allergy Immunol. 2008;145(4):277-82.

[4]. Non-clinical pharmacology, pharmacokinetics, and safety findings for the antihistamine bepotastine besilate. Curr Med Res Opin. 2010 Oct;26(10):2329-38.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H31CLN2O6S
Molecular Weight
547.06
Exact Mass
546.16
Elemental Analysis
C, 59.28; H, 5.71; Cl, 6.48; N, 5.12; O, 17.55; S, 5.86
CAS #
190786-44-8
Appearance
Solid powder
SMILES
C1CN(CCC1O[C@@H](C2=CC=C(C=C2)Cl)C3=CC=CC=N3)CCCC(=O)O.C1=CC=C(C=C1)S(=O)(=O)O
InChi Key
UDGHXQPQKQPSBB-BOXHHOBZSA-N
InChi Code
InChI=1S/C21H25ClN2O3.C6H6O3S/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;7-10(8,9)6-4-2-1-3-5-6/h1-2,4,6-9,12,18,21H,3,5,10-11,13-15H2,(H,25,26);1-5H,(H,7,8,9)/t21-;/m0./s1
Chemical Name
benzenesulfonic acid;4-[4-[(S)-(4-chlorophenyl)-pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid
Synonyms
TAU 284; Bepotastine besylate; bepotastine besilate; TAU-284; TAU284;Bepreve; Talion
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~109 mg/mL (~199.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.8280 mL 9.1398 mL 18.2795 mL
5 mM 0.3656 mL 1.8280 mL 3.6559 mL
10 mM 0.1828 mL 0.9140 mL 1.8280 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03932435 Completed Drug: Fisrt period TWLO_C
Other: Washout period
Healthy Dong-A ST Co., Ltd. April 23, 2019 Not Applicable
NCT01840605 Completed Drug: Bepotastine besilate
Drug: ketotifen fumarate
Dermatitis
Atopic
Mitsubishi Tanabe Pharma Corporation March 2013 Phase 3
NCT01753739 Completed Drug: Bepotastine besilate
Drug: Placebo
Seasonal Allergic Rhinitis Bausch & Lomb Incorporated January 2013 Phase 2
NCT01861522 Completed Drug: Bepotastine besilate
Drug: Placebo
Perennial Allergic Rhinitis Mitsubishi Tanabe Pharma
Corporation
April 2013 Phase 3
NCT01900054 Completed Drug: Bepotastine besilate Perennial Allergic Rhinitis Mitsubishi Tanabe Pharma
Corporation
June 2013 Phase 3
Biological Data
  • Bepotastine Besilate
    Concentration-dependent stimulation of P-gp ATPase activity in isolated membrane from human P-gp-expressing cells by bepotastine (A) and verapamil (B).Drug Metab Dispos.2006 May;34(5):793-9.
  • Bepotastine Besilate
    Brain penetration of [14C]bepotastine in P-gp KO and WT mice.Drug Metab Dispos.2006 May;34(5):793-9.
  • Bepotastine Besilate
    Intestinal absorption of [14C]bepotastine from various sites of gastrointestinal tract of rats.Drug Metab Dispos.2006 May;34(5):793
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