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ADRA1D receptor antagonist 1

目录号 : GC68627

ADRA1D receptor antagonist 1 是一个高效、选择性的,有口服活性的 α1D 肾上腺素受拮抗剂,Ki 值为 1.6 nM。

ADRA1D receptor antagonist 1 Chemical Structure

Cas No.:1191908-14-1

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5mg
¥4,320.00
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10mg
¥7,200.00
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Sample solution is provided at 25 µL, 10mM.

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ADRA1D receptor antagonist 1 is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM[1].

ADRA1D receptor antagonist 1 shows low hERG inhibition[1].
ADRA1D receptor antagonist 1 exhibits higher selectivity for α1D-AR over α1A- and α1B-ARs [1].

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[1].

Animal Model: Rat with bladder outlet obstruction (BOO)[1]
Dosage: 4.4 µg/kg
Administration: Intravenous injection
Result: Dose-dependently decreased the non-voiding bladder contractions during urinary storage phase in rats with BOO.

[1]. Sakauchi N, et al. Discovery of 5-Chloro-1-(5-chloro-2-(metlsulfonyl)benzyl)-2-imino-1,2-didropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ethe

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1 mg 5 mg 10 mg
1 mM 2.9656 mL 14.828 mL 29.656 mL
5 mM 0.5931 mL 2.9656 mL 5.9312 mL
10 mM 0.2966 mL 1.4828 mL 2.9656 mL
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