Tiotropium Bromide hydrate

Catalog No.S2547 Synonyms: BA 679BR

Tiotropium Bromide hydrate Chemical Structure

Molecular Weight(MW): 490.43

Tiotropium Bromide hydrate is a monohydrate of tiotropium bromide (Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist.

Size Price Stock Quantity  
In DMSO USD 240 In stock
USD 120 In stock
USD 370 In stock
USD 670 In stock
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Biological Activity

Description Tiotropium Bromide hydrate is a monohydrate of tiotropium bromide (Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist.
Targets
AChR [1]
In vitro

Tiotropium bromide is a potent muscarinic antagonist with equal affinity for M1-, M2- and M3-receptors and is approximately 10-fold more potent than ipratropium bromide. Tiotropium bromide has a potent inhibitory effect against cholinergic nerve-induced contraction of guinea-pig and human airways, that has a slower onset than atropine or ipratropium bromide. Tiotropium bromide, ipratropium bromide and atropine all increase ACh release on neural stimulation and that this effect is washed out equally quickly for the three antagonists. Tiotropium bromide dissociates slowly from M3-receptors (on airway smooth muscle) but rapidly from M2 autoreceptors (on cholinergic nerve terminals). [1] Tiotropium significantly inhibits the release of chemotactic substances by AM, MonoMac6 and A549 cells. [2] Tiotropium bromide inhibits the Th2 cytokine production from PBMCs. [3]

In vivo Tiotropium bromide significantly reduces airway inflammation and the Th2 cytokine production in bronchoalveolar lavage fluid (BALF) in both acute and chronic mouse models of asthma. Tiotropium bromide significantly decreases the goblet cell metaplasia, thickness of airway smooth muscle, and airway fibrosis in a mouse model of asthma. Tiotropium bromide reduces the levels of TGF-beta1 in BALF in a chronic model. [3] Tiotropium inhibits the increase in airway smooth muscle mass, myosin expression, and contractility in a guinea pig model of ongoing allergic asthma. [4] Tiotropium abrogates the LPS-induced increase in neutrophils, goblet cells, collagen deposition and muscularised microvessels in a guinea pig model of chronic obstructive pulmonary disease (COPD), but has no effect on emphysema. [5]

Protocol

Solubility (25°C)

In vitro DMSO 8 mg/mL (16.31 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 490.43
Formula

C19H22NO4S2.Br.xH2O

CAS No. 139404-48-1
Storage powder
in solvent
Synonyms BA 679BR

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03376932 Withdrawn Asthma GlaxoSmithKline January 18 2019 Phase 3
NCT03376932 Withdrawn Asthma GlaxoSmithKline January 18 2019 Phase 3
NCT03842839 Recruiting Airway Remodeling Guangzhou Institute of Respiratory Disease October 1 2018 Not Applicable
NCT03842839 Recruiting Airway Remodeling Guangzhou Institute of Respiratory Disease October 1 2018 Not Applicable
NCT03673670 Completed COPD Verona Pharma plc July 16 2018 Phase 2
NCT03673670 Completed COPD Verona Pharma plc July 16 2018 Phase 2

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AChR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID