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TD-5471 hydrochloride is a selective and potent long-acting human β2-adrenergic receptor agonist for the treatment of chronic obstructive pulmonary disease (COPD).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $700 | 6-8 weeks |
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]. |
Molecular Weight | 558.07 |
Formula | C32H32ClN3O4 |
Cas No. | 530084-35-6 |
Smiles | [C@@H](CNCCC1=CC=C(NC2=CC(=C(OC)C=C2)C3=CC=CC=C3)C=C1)(O)C4=C5C(=C(O)C=C4)NC(=O)C=C5.Cl |
Relative Density. | no data available |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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