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BEPOTASTINE BESILATE

Product Name
BEPOTASTINE BESILATE
CAS No.
190786-44-8
Chemical Name
BEPOTASTINE BESILATE
Synonyms
BB;CS-645;CS-487;Talion;Bepreve;TAU 284;Talion (TN);Benzestatine;Betastine besylate;BEPOTASTINE BESILATE
CBNumber
CB9810068
Molecular Formula
C27H31ClN2O6S
Formula Weight
547.06
MOL File
190786-44-8.mol
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BEPOTASTINE BESILATE Property

Melting point:
161-163°
alpha 
D20 +6.0° (c = 5 in methanol)
storage temp. 
Inert atmosphere,Room Temperature
solubility 
DMSO (Slightly, Heated), Methanol (Slightly, Heated)
form 
Solid
color 
White to Light Beige
Stability:
Hygroscopic
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
23721
Product name
Bepotastine (besylate)
Purity
≥95%
Packaging
5mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
23721
Product name
Bepotastine (besylate)
Purity
≥95%
Packaging
10mg
Price
$78
Updated
2024/03/01
Cayman Chemical
Product number
23721
Product name
Bepotastine (besylate)
Purity
≥95%
Packaging
25mg
Price
$172
Updated
2024/03/01
Usbiological
Product number
003877
Product name
Bepotastine Besylate
Packaging
5mg
Price
$425
Updated
2021/12/16
TRC
Product number
B317000
Product name
(S)-BepotastineBesylate
Packaging
50mg
Price
$280
Updated
2021/12/16
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BEPOTASTINE BESILATE Chemical Properties,Usage,Production

Description

Betotastine was introduced in Japan for the treatment of allergic rhinitis. This structurally-related derivative of chlorpheniramine and ebastine is prepared by condensation of optically-resolved 4-[1-(4-chlorophenyl)-1-(2-pyridyl)-methoxy]piperidine with ethyl 4-bromobutyrate followed by ester hydrolysis. Betotastine is the seventh marketed non-sedating histamine H1 antagonist. Its very low sedative side effect is due to very poor penetration in the central nervous system. Besides its potent and long-acting activity in models of allergic rhinitis, betotastine was also shown to act as a PAF antagonist and inhibit LTD4 in tracheal smooth muscle and ileum, IL-5 production by human peripheral blood mononuclear cells as well as eosinophil infiltration in the airway and peripheral blood. As a consequence, it is currently being developed against other allergic and respiratory disorders.

Description

Bepotastine is an antagonist of the histamine H1 receptor that is selective over H3, α1-, α2-, and β-adrenergic, dopamine D2long, serotonin 5-HT2, muscarinic acetylcholine, and benzodiazepine receptors. It reduces dye leakage from the nasal passages of rats acutely sensitized to an antigen (ED50 = 0.03 mg/kg) and inhibits histamine-induced bronchoconstriction in the anesthetized dog (ED50 = 3.2 μg/kg). Bepotastine prevents conjunctival vascular hyperpermeability in a guinea pig model of conjunctivitis in a dose-dependent manner. Formulations containing bepotastine have been used in the treatment of itching associated with allergic conjunctivitis.

Chemical Properties

Off-White to Light Beige Solid

Originator

UBE (Japan)

Uses

Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7

Uses

Bepotastine is a histamine H1 receptor anatagonist. Bepotastine suppresses some allergic inflammatory processes such as allergic rhinitis, chronic urticaria or pruritus associated with skin conditions (eczema/dermatitis, prurigo or pruritus cutaneus).

Definition

ChEBI: An organosulfonate salt obtained by combining equimolar amounts of bepotastine and benzenesulfonic acid. A topical, selective and non-sedating histamine (H1) receptor antagonist used for treatment of itching associated with allergic co junctivitis.

Manufacturing Process

Manufacturing process for BEPOTASTINE BESILATE includes these steps as follows: Step A: Synthesis of Methyl 2-endo-hydroxy-1-exo-hydroxymethyl-3a,8b-cis-2,3,3a,8b-tetrahydro- 1H-5-cyclopenta[b]benzofurancarboxylate,Step B: Synthesis of Methyl 3-methyl-trans-4a-cisoid-4a,5a-cis-5a-1,4a,5,5a,10b,10c-hexahydro-7- dioxin o[5,4-a]cyclopenta[b]benzofurancarboxylate,Step C: Synthesis of 3-Methyl-trans-4a-cosoid-4a,5a-cis-5a-1,4a,5,5a,10b,10c-hexahydro-7- dioxino[5,4-a]cyclopenta[b]benzofuranylmethanol,Step D: Synthesis of 7-Chloromethyl-3-methyl-trans-4a-cisoid-4a,5a-cis-5a-1,4a,5,5a,10b,10chexahydrodioxino[5,4-a]cyclopenta[b]benzofuran,Step E: Synthesis of 4-[3-Methyl-trans-4a-cisoid-4a,5a-cis-5a-1,4a,5,5a,10b,10c-hexahydro-7- dioxino[5,4-a]cyclopenta[b]benzofuranyl]butyric acid, Step F: Synthesis of Methyl 4-[2-endo-hydroxy-1-exo-hydroxymethyl-3a,8b-cis-2,3,3a,8btetrahydro-1H-5- cyclopenta[b]benzofuranyl]butyrate, Step G: Synthesis of Methyl 4-[2-endo-acetoxy-1-exo-hydroxymethyl-3a,8b-cis-2,3,3a,8btetrahydro-1H-5-cyclopenta[b]benzofuranyl]butyrate, Step H: Synthesis of Methyl ester of 11,15-dideoxy-11-acetoxy-16-methyl-15-oxo-18,19- tetradehydro-5,6,7-trinor-4,8-inter-m-phenylene PGI2,Step I: Synthesis of 11-Deoxy-11-acetoxy-16-methyl-18,19-tetradehydro-5,6,7-trinor-4,8-inter-mphenylene PGI2.To a solution of 54 mg of methyl ester of 11-deoxy-11-acetoxy-16-methyl- 18,19-tetradehydro-5,6,7-trinor-4,8-inter-m-phenylene PGI2 in 4.5 ml of anhydrous methanol was added 0.001 ml of 4.8 N sodium methoxide under argon, and the reaction mixture was stirred for 1.5 hours at room temperature. After addition of acetic acid to the reaction mixture and concentration of the mixture, the residue was dissolved in 20 ml of ethyl acetate, and the solution was washed with aqueous saturated solution of sodium hydrogen carbonate, water and aqueous saturated solution of sodium chloride, dried and concentrated to afford 55 mg of an oily material. This oily material was purified by column chromatography using ethyl acetate and cyclohexane (3:1) as eluent to give 48 mg of the methyl ester of 16- methyl-18,19-tetradehydro-5,6,7-trinor-4,8-inter-m-phenylene PGI2.

brand name

Talion

Therapeutic Function

Antiallergic

BEPOTASTINE BESILATE Preparation Products And Raw materials

Raw materials

Preparation Products

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BEPOTASTINE BESILATE Suppliers

Canada 1 China 232 India 19 Japan 2 Spain 1 United Kingdom 4 United States 23 Global 282
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View Lastest Price from BEPOTASTINE BESILATE manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Bepotastine besylate 190786-44-8
Price
US $0.00-0.00/g
Min. Order
1g
Purity
98.0%
Supply Ability
1kg/month
Release date
2021-09-26
Hebei Chuanghai Biotechnology Co,.LTD
Product
Bepotastine Besilate 190786-44-8
Price
US $10.70/KG
Min. Order
10KG
Purity
99%
Supply Ability
10000kg
Release date
2024-08-21
Henan Bao Enluo International TradeCo.，LTD
Product
BEPOTASTINE BESILATE 190786-44-8
Price
US $30.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
1000tons
Release date
2023-07-25

190786-44-8, BEPOTASTINE BESILATERelated Search:

sodium phenyl sulfate Isopropyl Benzenesulfonate Butyl Benzenesulfonate 2-hydroxyethyl benzenesulfonate Methyl benzenesulfonate Ramelteon 2-[(S)-(4-Chlorophenyl)(4-piperidinyloxy)methyl]pyridine (2R,3R)-2,3-Dihydroxybutanedioate 4-[(4-Chlorophenyl)-2-pyridinylmethoxy]-1-piperidinebutanoic acid Bepotastine Ethyl Ester 1-Piperidinebutanoic acid, 4-[(4-chlorophenyl)-2-pyridinylmethoxy]-, (R)- Fasudil hydrochloride FMOC-GLY-GLY-GLY-OH 5-alpha-Hydroxy- Laxogenin 5-[Bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazole-2-butanoic acid ethyl ester 1-Methyl-5-amino-1H-benzimidazole-2-butanoic acid ethyl ester ethyl 4-(1-methyl-5-nitro-1H-benzo[d]imidazol-2-yl)butanoate Benzenesulfonamide Ethyl benzenesulphonate

  • BEPOTASTINE BESILATE
  • (+)-(S)-4-(4-((4-Chlorophenyl)(2-pyridyl)methoxy)piperidino)butyric acid monobenzenesulfonate
  • 4-((4-Chlorophenyl)-2-pyridinylmethoxy)- (S)-1-piperidinebutanoic acid monobenzenesulfonate
  • Talion (TN)
  • Bepotastine Beslilat
  • Bepotastine Besylate
  • 1-Piperidinebutanoic acid, 4-[(4-chlorophenyl)-2-pyridinylmethoxy]-, (S)-, monobenzenesulfonate
  • 1-Piperidinebutanoic acid, 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-, monobenzenesulfonate
  • 4-[4-[(R)-(4-chlorophenyl)-pyridin-2-yl-methoxy]-1-piperidyl]butanoic acid
  • (+)-(S)-4-[4-[1-(4-Chlorophenyl)-1-(2-pyridyl)methoxy]piperidin-1-yl]butyric acid benzenesulfonate
  • Benzestatine
  • CS-645
  • CS-487
  • bepotastine benzenesulfonate salt
  • (S)-4-[4-(4-Chlorophenyl-2-pyridylMethoxy)piperidinyl]butyric Acid Benzenesulfonate
  • 4-[(S)-(4-Chlorophenyl)-2-pyridinylMethoxy]-1-piperidinebutanoic Acid Benzenesulfonate
  • BB
  • Bepotastine Benzenesulfonate
  • Bepreve
  • Talion
  • TAU 284
  • Bepotastine Beslilate
  • 4-[4-[(4-chlorophenyl)-pyridin-2-ylMethoxy]piperidin-1-yl]butanoic acid benzenesulfonate
  • 1-Piperidinebutanoic acid, 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-, benzenesulfonate (1:1)
  • Benzenesulfonate salt
  • (S)-Bepotastine Besylate
  • Bepotastine Besilate (This product is only available in Japan.)
  • (S)-4-[4-[(4-Chlorophenyl)(pyridin-2-yl)methoxy]piperidin-1-yl]butanoic Acid Benzenesulfonate
  • 4-[4-[(S)-(4-Chlorophenyl)(2-pyridinyl)methoxy]-1-piperidinyl]butanoic Acid Benzenesulfonate
  • BEPOTASTINE BESILATE USP/EP/BP
  • Betastine besylate
  • Bepotastine Besilate (Bepreve)
  • Bepotastine BesilateQ: What is Bepotastine Besilate Q: What is the CAS Number of Bepotastine Besilate Q: What is the storage condition of Bepotastine Besilate Q: What are the applications of Bepotastine Besilate
  • (S)-4-(4-((4-Chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl)butanoic acid compound with benzenesulfonic acid (1:1)
  • (S)-4-(4-((4-chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl)butanoic acid, benzenesulfonic acid
  • 190786-44-8
  • C21H25ClN2O3C6H6O3S
  • C27H31ClN2O6S
  • 54706
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