Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Bepotastine (also known as TAU 284; Bepreve) is a second generation, non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. Bepostatine besilate is used to relieve pruritus, urticaria, and allergic rhinitis. By inhibiting histamine H1 receptors, bepotastine besilate counteracts the effects of histamine on the vasoconstrictor and, to a lesser extent, the vasodilator. By severing the regular flow of intracellular signals, mast cell stabilisers prevent degranulation and the subsequent release of histamine. Talion represents the brand of bepostatine besilate.
Targets |
Histamine H1 receptor
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ln Vitro |
Bepotastine (10, 100, 1000 µM; preincubates for 120 min) reduces the amount of histamine released when treated with A23187, reaching a statistically significant level at 1000 µM[1].
Bepotastine (50 µM; 1 h) inhibits the expression of NGF mRNA in NHEKs[2]. |
ln Vivo |
Bepotastine (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) significantly reduces the infiltration of conjunctival eosinophils induced by PAF[1].
Bepotastine (3 mg/kg; p.o.; once) minimizes scratching to a frequency of 59.0 and a duration of 14.57 seconds, which is nearly identical to the control[3]. Bepotastine (10 mg/kg; p.o.; once) significantly suppresses 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: RPMCs
Concentration: 10, 100, 1000 µM Incubation Time: 120 min (preincubate) Result: Decreased the release of histamine |
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 |
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Molecular Formula |
C21H25CLN2O3
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Molecular Weight |
388.8878
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Exact Mass |
388.16
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Elemental Analysis |
C, 64.86; H, 6.48; Cl, 9.12; N, 7.20; O, 12.34
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CAS # |
125602-71-3
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Related CAS # |
Bepotastine besilate; 190786-44-8; Bepotastine tosylate; 1160415-45-1; 125602-71-3
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Appearance |
Solid powder
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SMILES |
C1CN(CCC1O[C@@H](C2=CC=C(C=C2)Cl)C3=CC=CC=N3)CCCC(=O)O
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InChi Key |
YWGDOWXRIALTES-NRFANRHFSA-N
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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)/t21-/m0/s1
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Chemical Name |
4-[4-[(S)-(4-chlorophenyl)-pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid
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Synonyms |
TAU-284; TAU 284; TAU284; Bepotastine band name: Talion; Bepreve
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 78~100 mg/mL (200.6~257.1 mM)
Water: ~78 mg/mL Ethanol: ~78 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5714 mL | 12.8571 mL | 25.7142 mL | |
5 mM | 0.5143 mL | 2.5714 mL | 5.1428 mL | |
10 mM | 0.2571 mL | 1.2857 mL | 2.5714 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.
Calculation results
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.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01900054 | Completed | Drug: Bepotastine besilate | Perennial Allergic Rhinitis | Mitsubishi Tanabe Pharma Corporation |
June 2013 | Phase 3 |
NCT01861522 | Completed | Drug: Bepotastine besilate Drug: Placebo |
Perennial Allergic Rhinitis | Mitsubishi Tanabe Pharma Corporation |
April 2013 | Phase 3 |
NCT01840605 | Completed | Drug: Bepotastine besilate Drug: ketotifen fumarate |
Dermatitis Atopic |
Mitsubishi Tanabe Pharma Corporation |
March 2013 | Phase 3 |
NCT01425632 | Completed | Drug: TAU-284 Drug: Placebo |
Perennial Allergic Rhinitis | Mitsubishi Tanabe Pharma Corporation |
August 2011 | Phase 3 |
NCT00586625 | Completed | Drug: Bepreve Drug: Placebo |
Allergic Conjunctivitis | Bausch & Lomb Incorporated | October 2007 | Phase 3 |