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    Tiotropium Bromide hydrate (BA-679 BR)
    Tiotropium Bromide hydrate (BA-679 BR)

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V1160
    CAS #: 139404-48-1Purity ≥98%

    Description: Tiotropium Bromide hydrate (PUR-0200; BA-679BR; BA679BR; PUR0200; Spiriva), the monohydrate form of tiotropium bromide, is an anticholinergic and bronchodilator and a muscarinic receptor antagonist used as a long-acting bronchodilator for the management of chronic obstructive pulmonary disease (COPD).  

    References: Respir Med. 2007 Nov;101(11):2386-94; Clin Exp Allergy. 2010 Aug;40(8):1266-75.

    Related CAS #:136310-93-5 [Tiotropium Bromide (BA679 BR)]

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    Molecular Weight (MW)490.43
    FormulaC19H22NO4S2.Br.xH2O
    CAS No.139404-48-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 8 mg/mL (16.3 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical 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
    InChi Key: DQHNAVOVODVIMG-RGECMCKFSA-M
    InChi Code: InChI=1S/C19H22NO4S2.BrH/c1-20(2)12-9-11(10-13(20)17-16(12)24-17)23-18(21)19(22,14-5-3-7-25-14)15-6-4-8-26-15;/h3-8,11-13,16-17,22H,9-10H2,1-2H3;1H/q+1;/p-1/t11?,12-,13+,16-,17+;
    SMILES Code: C[N+]1([[email protected]@H]2CC(C[[email protected]]1[[email protected]]3[[email protected]@H]2O3)OC(=O)C(C4=CC=CS4)(C5=CC=CS5)O)C.[Br-]
    SynonymsBA 679BR; PUR-0200; BA 679BR; BA-679BR; BA679BR; PUR0200; PUR 0200; Tiotropium bromide, trade name: Spiriva.


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    In Vitro

    In vitro activity: 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). Tiotropium significantly inhibits the release of chemotactic substances by AM, MonoMac6 and A549 cells. Tiotropium bromide inhibits the Th2 cytokine production from PBMCs.


    Kinase Assay: Tiotropium Bromide hydrate is an anticholinergic and bronchodilator and a muscarinic receptor antagonist. Target: mAChR Tiotropium 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). 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.

    In VivoTiotropium 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. Tiotropium inhibits the increase in airway smooth muscle mass, myosin expression, and contractility in a guinea pig model of ongoing allergic asthma. 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.
    Animal modelacute and chronic mouse models of asthma
    Formulation & DosageN/A
    ReferencesRespir Med. 2007 Nov;101(11):2386-94; Clin Exp Allergy. 2010 Aug;40(8):1266-75.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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