(R)-9s

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency: 

Ki

1.9 nM

Potency assay: 

Cell Free Activity Assay

Off target activity

Potency assay (off target): 

Binding to ADRA1A > 1700 fold, binding to ADRA1B > 750 fold

Probe Selectivity in Vitro: 

unknown selectivity outside target family

In cell validation

On target activity in cells

Potency in cells: 

IC30

15 nM

Potency assay (cells): 

Organ bath

In vivo validation

Organism: 

Rat

Dose: 

1 mg/kg

Route of delivery: 

Oral

Other route of delivery: 

I.V.

Plasma half life: 

4.14 h

Fraction of probe bound to plasma protein: 

86%

Cmax: 

142ng/ml

Organ of Interest

Organ (O): 

Bladder