TD-5471 hydrochloride 

TD-5471 hydrochloride is a potent and selective full agonist of the human β₂-adrenoceptor.

TD-5471 is potent, with slow onset in an in vitro guinea pig trachea model. TD-5471 has potency with pEC₅₀ of 8.7 in the guinea pig tracheal ring assay.TD-5471 is structurally differentiated from Milveterol and its long duration of action is consistent with a correlation with hydrophobicity observed in other long-acting β₂-agonist discovery programs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TD-5471 shows a dose-dependent and long duration of action in an in vivo guinea pig model of bronchoprotection. In a guinea pig model of in vivo bronchoprotection, TD-5471 shows excellent potency (measured 1.5 h after nebulized dosing). Because a high dose of Salmeterol (300 μg/mL) provides bronchoprotection lasting ≥24 h in this model, a 72 h time point is selected to provide confidence that TD-5471 will be suitable for once-daily dosing in man. TD-5471-mediated bronchoprotection at 72 h is dose-dependent and is significantly greater than that of Salmeterol at nebulizer concentrations of ≥30 μg/mL^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

558.07

C₃₂H₃₂ClN₃O₄

530084-35-6

O=C1NC2=C(C([C@@H](O)CNCCC3=CC=C(NC4=CC(C5=CC=CC=C5)=C(OC)C=C4)C=C3)=CC=C2O)C=C1.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Jacobsen JR, et al. Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2625-30.  [Content Brief]