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TD-5471 hydrochloride

TD-5471 hydrochloride
TD-5471 hydrochloride is a selective and potent long-acting human β2-adrenergic receptor agonist for the treatment of chronic obstructive pulmonary disease (COPD).
Catalog No. T13106Cas No. 530084-35-6
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Purity:99.57%
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TD-5471 hydrochloride

Catalog No. T13106Cas No. 530084-35-6
TD-5471 hydrochloride is a selective and potent long-acting human β2-adrenergic receptor agonist for the treatment of chronic obstructive pulmonary disease (COPD).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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1 mg$7006-8 weeks
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Product Introduction

Bioactivity
Description
TD-5471 hydrochloride is a selective and potent long-acting human β2-adrenergic receptor agonist for the treatment of chronic obstructive pulmonary disease (COPD).
Targets&IC50
guinea pig trachea:8.7 (pEC50)
In vitro
In an in vitro guinea pig trachea model, TD-5471 exhibits potent activity with a slow onset. Its potency is evident, as indicated by a pEC50 of 8.7 in the guinea pig tracheal ring assay. Notably, TD-5471 is structurally distinct from Milveterol, and its prolonged duration of action aligns with a correlation observed in other long-acting β2-agonist discovery programs, specifically related to hydrophobicity[1].
In vivo
In an in vivo guinea pig model of bronchoprotection, TD-5471 demonstrates a prolonged and dose-dependent duration of action. The efficacy of TD-5471 is notably high, as evidenced by its excellent potency measured 1.5 hours after nebulized dosing. To ensure suitability for once-daily dosing in humans, a 72-hour time point is chosen, considering that a high dose of Salmeterol (300 μg/mL) provides bronchoprotection lasting ≥24 hours in this model.
At the 72-hour time point, TD-5471-mediated bronchoprotection remains dose-dependent and significantly surpasses the efficacy of Salmeterol at nebulizer concentrations of ≥30 μg/mL[1].
Chemical Properties
Molecular Weight558.07
FormulaC32H32ClN3O4
Cas No.530084-35-6
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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