PKG drug G1 靶向作用于PKG Iα。它通过 C42 PKGIα 非依赖性机制，促进血管舒张以及血压降低。

PKG drug G1 targets PKG Iα C42. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

The absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys. The metabolism of Asimadoline is rapid and appears similar in animals and man. Asimadoline has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels

Mice constitutively expressing PKG Iα Cys42Ser are generated on a pure C57BL/6 background. Age-matched and. body weight–matched WT or PKG Iα Cys42Ser KI male mice are used in all studies. Blood pressure and heart rate are. assessed by radio telemetry in conscious freely moving mice. Alzet osmotic mini-pumps are used to deliver. angiotensin II at 1.1 mg/kg per day in some studies. PKG drug G1 is delivered intraperitoneally (3.7-14.8 mg/kg) or. orally (20 mg/kg) in some studies. To deliver PKG drug G1 orally, without stress or risk of dislodging the telemetric. probe catheter, it is provided suspended in water and set in gelatin flavored with sodium saccharin.

374703-78-3

C13H11N3OS

257.31

DMSO:103 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years