| Description |
Remikiren (Ro 42-5892) is an orally active and highly specific renin inhibitor. Remikiren specifically inhibits human reninand human plasma renin with IC50 values of 0.7 and 0.8 nM, respectively. Remikiren also reduces mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys. Remikiren can be used in study of hypertension[1].
|
| Related Catalog |
|
| Target |
IC50:0.7 nM (human pure renin), 0.8 nM (plasma renin of human)[1].
|
| In Vitro |
Remikiren (0-10 nM; 1-3 h) displays a considerable specificity to inhibit renin[1]. Cell Viability Assay[1] Cell Line: Human pure renin, plasma renin of human, marmoset, squirrel monkey Concentration: 0-10 nM Incubation Time: 1-3 h Result: Inhibited human pure renin and plasma renin of human, marmoset, squirrel monkey with IC50 values of 0.7, 0.8, 1.0 and 1.7 nM, respectively.
|
| In Vivo |
Remikiren (0.1, 0.3, 1, 3, 10 mg/kg; p.o.; single) reduces mean arterial blood pressure in a dose-dependent manner in sodium-depleted marmosets and squirrel monkeys[1]. Remikiren (3 mg/kg; p.o.; single) shows the duration of blood pressure decrease more than 24 h in sodium-depleted marmosets[1]. Animal Model: Marmosets and squirrel monkeys (sodium-depleted)[1]. Dosage: 0.1, 0.3, 1, 3, 10 mg/kg Administration: Oral administration; single. Result: Decreased mean arterial pressure (MAP) by 20-25 mm Hg when at 0.1 mg/kg. Reached the maximal decrease (30 mm Hg) of MAP with 1 mg/kg in marmosets. Decreasesd 35 mm Hg blood pressure with 3-10 mg/kg in squirrel monkeys. Animal Model: Marmosets (sodium-depleted)[1]. Dosage: 3 mg/kg Administration: Oral administration; single. Result: Showed MAP fell by 30 mm Hg, which lasting more than 24 h.
|
