PeptideDB

ADRA1D receptor antagonist 1

CAS: 1191908-14-1 F: C15H14Cl2N4O W: 337.20

ADRA1D receptor antagonist 1 is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM.
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Bioactivity ADRA1D receptor antagonist 1 is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM[1].
Target Ki: 1.6 nM (α1D adrenoceptor)
Invitro 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].
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[1]. Animal Model:
Name ADRA1D receptor antagonist 1
CAS 1191908-14-1
Formula C15H14Cl2N4O
Molar Mass 337.20
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

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)

Reference [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