Tiotropium Bromide hydrate

Synonyms: BA 679BR

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

Tiotropium Bromide hydrate Chemical Structure

Tiotropium Bromide hydrate Chemical Structure

CAS No. 139404-48-1

Purity & Quality Control

Tiotropium Bromide hydrate Related Products

Signaling Pathway

Biological Activity

Description Tiotropium Bromide hydrate (BA 679BR) 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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05246046 Completed
Healthy Volunteers
Orion Corporation Orion Pharma
February 16 2022 Phase 1
NCT04990167 Recruiting
Asthma in Children
Nemours Children''s Clinic
January 1 2022 Phase 2
NCT05295355 Recruiting
Chronic Obstructive Pulmonary Disease
Guangzhou Institute of Respiratory Disease|Boehringer Ingelheim
January 25 2021 Not Applicable
NCT04999930 Completed
Chronic Obstructive Pulmonary Disease
National University of Malaysia
January 10 2020 Not Applicable

Chemical Information & Solubility

Molecular Weight 490.43 Formula

C19H22NO4S2.Br.xH2O

CAS No. 139404-48-1 SDF Download Tiotropium Bromide hydrate SDF
Smiles C[N+]1(C2CC(CC1C3C2O3)OC(=O)C(C4=CC=CS4)(C5=CC=CS5)O)C.O.[Br-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 8 mg/mL ( (16.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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