| Bioactivity | TD-5471 hydrochloride is a potent and selective full agonist of the human β2-adrenoceptor. |
| Invitro | 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]. |
| In Vivo | 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]. |
| Name | TD-5471 hydrochloride |
| CAS | 530084-35-6 |
| Formula | C32H32ClN3O4 |
| Molar Mass | 558.07 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |