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Tiotropium Bromide hydrate

Catalog No.GC13134 Copy One-Click Copy Product Info

Muscarinic antagonist

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Tiotropium Bromide hydrate Chemical Structure

Cas No.: 139404-48-1

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100mg
$95.00
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Sample solution is provided at 25 µL, 10mM.



Description of Tiotropium Bromide hydrate

Tiotropium Bromide hydrate is an anticholinergic and bronchodilator and a muscarinic receptor antagonist.Target: mAChRTiotropium bromide (Ba 679 BR) is a novel potent and long-lasting muscarinic antagonist that has been developed for the treatment of chronic obstructive airways disease (COPD). Binding studies with [3H]tiotropium bromide in human lung have confirmed that this is a potent muscarinic antagonist with equal affinity for M1-, M2- and M3-receptors and is approximately 10-fold more potent than ipratropium bromide. In vitro 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 dissociates slowly from M3-receptors (on airway smooth muscle) but rapidly from M2 autoreceptors (on cholinergic nerve terminals) [1]. Tiotropium bromide is a quaternary ammonium derivative that binds to muscarinic receptors. However, although tiotropium binds with high affinity to muscarinic receptors of M1-, M2- and M3-subtypes, it dissociates very slowly from M1- and M3-receptors but more rapidly from M2-receptors, thereby giving it a unique kinetic selectivity [2].

References:
[1]. Barnes, P.J., et al., Tiotropium bromide (Ba 679 BR), a novel long-acting muscarinic antagonist for the treatment of obstructive airways disease. Life Sci, 1995. 56(11-12): p. 853-9.
[2]. Hansel, T.T. and P.J. Barnes, Tiotropium bromide: a novel once-daily anticholinergic bronchodilator for the treatment of COPD. Drugs Today (Barc), 2002. 38(9): p. 585-600.

Chemical Properties of Tiotropium Bromide hydrate

Cas No. 139404-48-1 SDF
Chemical Name (1R,2R,4S,5S,7s)-7-(2-hydroxy-2,2-di(thiophen-2-yl)acetoxy)-9,9-dimethyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-9-ium bromide hydrate
Canonical SMILES O=C(C(C1=C([H])C([H])=C([H])S1)(C2=C([H])C([H])=C([H])S2)O[H])O[C@@]3([H])C([H])([H])[C@]4([H])[N+](C([H])([H])[H])(C([H])([H])[H])[C@@](C3([H])[H])([H])[C@@]5([H])O[C@@]45[H].[H]O[H].[Br-]
Formula C19H22NO4S2.Br.xH2O M.Wt 490.43
Solubility DMSO : 8mg/mL Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Tiotropium Bromide hydrate

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1 mg 5 mg 10 mg
1 mM 2.039 mL 10.1951 mL 20.3903 mL
5 mM 407.8 μL 2.039 mL 4.0781 mL
10 mM 203.9 μL 1.0195 mL 2.039 mL
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In vivo Formulation Calculator (Clear solution) of Tiotropium Bromide hydrate

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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 saline, 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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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Review for Tiotropium Bromide hydrate

Average Rating: 5 ★★★★★ (Based on Reviews and 25 reference(s) in Google Scholar.)

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