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编 号：F745775
分子式：C24H28N2O6
分子量：440.49
分子式：C24H28N2O6
分子量：440.49
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CAS No: 1548286-45-8
产品详情
生物活性：
MK-8153 is a potent, selective and orally active inhibitor of renal outer medullary potassium channel (ROMK), with IC50s of 5 nM, 34 μM for ROMK electrophysiology (EP) and hERG EP, respectively. MK-8153 can be used as the diuretic/atriuretic.
体内研究：
MK-8153 (0.1-10 mg/kg/d, p.o. once daily for 3 days) causes a dose-dependent decrease in systolic blood pressure of aged SHRs. MK-8153 shows diuretic effects in SHRs.MK-8153 (2 mg/kg; p.o.) exhibits terminal elimination half-lives (rat 3.6, dog 9.1, Rhesus 3.3 h), bioavailability (rat 53%, dog ~100%, Rhesus 3.4%), and plasma clearance (rat 29.4, dog 8.7, Rhesus 58.3 mL/min/kg).Animal Model:Aged spontaneously hypertensive rats (SHRs)
Dosage:0.1, 0.3, 1, 3, 10 mg/kg
Administration:P.o. once daily for 3 days
Result:Observed the maximal lowering of systolic blood pressure (～24 mm Hg) by day 3 at the 3 mg/kg.Dose-dependently increased the sodium excretion.
体外研究：
MK-8153 inhibits current through rat ROMK, rKir1.1/HEK293 cells in electrophysiological recordings with an IC50 of 2.5 nM.
MK-8153 is a potent, selective and orally active inhibitor of renal outer medullary potassium channel (ROMK), with IC50s of 5 nM, 34 μM for ROMK electrophysiology (EP) and hERG EP, respectively. MK-8153 can be used as the diuretic/atriuretic.
体内研究：
MK-8153 (0.1-10 mg/kg/d, p.o. once daily for 3 days) causes a dose-dependent decrease in systolic blood pressure of aged SHRs. MK-8153 shows diuretic effects in SHRs.MK-8153 (2 mg/kg; p.o.) exhibits terminal elimination half-lives (rat 3.6, dog 9.1, Rhesus 3.3 h), bioavailability (rat 53%, dog ~100%, Rhesus 3.4%), and plasma clearance (rat 29.4, dog 8.7, Rhesus 58.3 mL/min/kg).Animal Model:Aged spontaneously hypertensive rats (SHRs)
Dosage:0.1, 0.3, 1, 3, 10 mg/kg
Administration:P.o. once daily for 3 days
Result:Observed the maximal lowering of systolic blood pressure (～24 mm Hg) by day 3 at the 3 mg/kg.Dose-dependently increased the sodium excretion.
体外研究：
MK-8153 inhibits current through rat ROMK, rKir1.1/HEK293 cells in electrophysiological recordings with an IC50 of 2.5 nM.
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