530084-35-6

530084-35-6 structure

Name: TD-5471 hydrochloride
Chemical Name: TD-5471 hydrochloride
CAS Number: 530084-35-6
Molecular Formula: C₃₂H₃₂ClN₃O₄
Molecular Weight: 558.067
Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
Create Date: 2018-06-26 01:39:25
Modify Date: 2024-01-10 06:33:57
TD-5471 hydrochloride is a potent and selective full agonist of the human β2-adrenoceptor.

Name	TD-5471 hydrochloride
Synonyms	2(1H)-Quinolinone, 8-hydroxy-5-[(1R)-1-hydroxy-2-[[2-[4-[(6-methoxy[1,1'-biphenyl]-3-yl)amino]phenyl]ethyl]amino]ethyl]-, hydrochloride (1:1) 8-Hydroxy-5-{(1R)-1-hydroxy-2-[(2-{4-[(6-methoxy-3-biphenylyl)amino]phenyl}ethyl)amino]ethyl}-2(1H)-quinolinone hydrochloride (1:1)

Description	TD-5471 hydrochloride is a potent and selective full agonist of the human β2-adrenoceptor.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Metabolic Disease
Target	β2 adrenoceptor[1]
In Vitro	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].
References	[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.