TD-5471 hydrochloride |
| カタログ番号GC31453 |
TD-5471 塩酸塩は、ヒト β2 アドレナリン受容体の強力かつ選択的な完全アゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 530084-35-6
Sample solution is provided at 25 µL, 10mM.
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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].
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].
[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.
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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