TD-5471 hydrochloride

Names

[ CAS No. ]:
530084-35-6

[ Name ]:
TD-5471 hydrochloride

[Synonym ]:
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)

Biological Activity

[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.


[Related Small Molecules]

Isoprenaline hydrochloride | ICI 118,551 (hydrochloride) | Phenylephrine hydrochloride | Yohimbine hydrochloride | Adrenaline | Ivabradine hydrochloride | Prazosin hydrochloride | Clenbuterol hydrochloride | Phentolamine mesilate | guanfacine hydrochloride | pimozide | Sotalol hydrochloride | Carvedilol | Atenolol | Metroprolol succinate

Chemical & Physical Properties

[ Molecular Formula ]:
C32H32ClN3O4

[ Molecular Weight ]:
558.067

[ Exact Mass ]:
557.208130

Related Compounds