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BEPOTASTINE BESILATE

CAS No.
190786-44-8
Chemical Name:
BEPOTASTINE BESILATE
Synonyms
BB;Talion;CS-645;CS-487;Bepreve;TAU 284;Talion (TN);Benzestatine;Betastine besylate;Bepotastine Besylate
CBNumber:
CB9810068
Molecular Formula:
C27H31ClN2O6S
Molecular Weight:
547.06
MDL Number:
MFCD01938491
MOL File:
190786-44-8.mol
Last updated:2023-07-25 15:04:37

BEPOTASTINE BESILATE Properties

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
FDA UNII 6W18MO1QR3

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338
NFPA 704
0
2 0

BEPOTASTINE BESILATE price More Price(40)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 23721 Bepotastine (besylate) ≥95% 190786-44-8 5mg $44 2024-03-01 Buy
Cayman Chemical 23721 Bepotastine (besylate) ≥95% 190786-44-8 10mg $78 2024-03-01 Buy
Cayman Chemical 23721 Bepotastine (besylate) ≥95% 190786-44-8 25mg $172 2024-03-01 Buy
Usbiological 003877 Bepotastine Besylate 190786-44-8 5mg $425 2021-12-16 Buy
TRC B317000 (S)-BepotastineBesylate 190786-44-8 50mg $280 2021-12-16 Buy
Product number Packaging Price Buy
23721 5mg $44 Buy
23721 10mg $78 Buy
23721 25mg $172 Buy
003877 5mg $425 Buy
B317000 50mg $280 Buy

BEPOTASTINE BESILATE Chemical Properties,Uses,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 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).

Uses

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

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

Global( 278)Suppliers
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Henan Bao Enluo International TradeCo.,LTD
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Capot Chemical Co.,Ltd.
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Henan Tianfu Chemical Co.,Ltd.
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Nanjing ChemLin Chemical Industry Co., Ltd.
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025-85710122 17714198479 sales@fine-chemtech.com CHINA 885 55
career henan chemical co
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Shenzhen Nexconn Pharmatechs Ltd
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HubeiwidelychemicaltechnologyCo.,Ltd
18627774460 faith@widelychemical.com CHINA 742 58

View Lastest Price from BEPOTASTINE BESILATE manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
BEPOTASTINE BESILATE pictures 2023-07-26 BEPOTASTINE BESILATE
190786-44-8
US $30.00 / kg 1kg 99% 1000tons Henan Bao Enluo International TradeCo.,LTD
Bepotastine Besilate pictures 2023-04-20 Bepotastine Besilate
190786-44-8
US $50.00 / kg 1kg 99% 100 tons Hebei Duling International Trade Co. LTD
Bepotastine Besilate pictures 2023-03-06 Bepotastine Besilate
190786-44-8
US $10.70 / Kg/Bag 10g 99% 10000kg Hebei Guanlang Biotechnology Co,.LTD

BEPOTASTINE BESILATE Spectrum

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 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 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 (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 Benzestatine CS-645 CS-487 (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 Inhibitors Other APIs Aromatics Drug Analogues Heterocycles Intermediates & Fine Chemicals Pharmaceuticals API Amino Acids & Derivatives Coronavirus