ADRA1D receptor antagonist 1 (free base)

ADRA1D receptor antagonist 1 (free base) (compound (R) -9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM) . ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.

Product Specifications

CAS Number

[1191908-24-3]

UNSPSC

12352005

Target

Adrenergic Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Endocrinology

Assay Protocol

https://www.medchemexpress.com/adra1d-receptor-antagonist-1-free-base.html

Solubility

10 mM in DMSO

Smiles

O=C(C1=CC(Cl)=CN([C@@H](C2=CC=CC(C#N)=C2)C)C1=N)N

Molecular Formula

C15H13ClN4O

Molecular Weight

300.74

References & Citations

[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 Ether-a-go-go-Related Gene (hERG) Liabilities. J Med Chem. 2016 Apr 14;59 (7) :2989-3002.