ADRA1D receptor antagonist 1 is a potent, selective and orally active α 1D adrenoceptor antagonist, with a K i of 1.6 nM.
性状
Solid
IC50 & Target[1][2]
Ki: 1.6 nM (α1D adrenoceptor)
体外研究(In Vitro)
ADRA1D receptor antagonist 1 shows low hERG inhibition.ADRA1D receptor antagonist 1 exhibits higher selectivity for α1D-AR over α1A- and α1B-ARs . has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ADRA1D receptor antagonist 1 (4.4 μg/kg; i.v.) dose-dependently decreases the non-voiding bladder contractions during the urinary storage phase in rats with BOO. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Sakauchi N, et al. Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ethe
溶解度数据
In Vitro: DMSO : 100 mg/mL (296.56 mM; Need ultrasonic)配制储备液