MK-8153 是一种有效的，选择性和具有口服活性的肾外髓质钾通道 (ROMK) 抑制剂，对 ROMK EP 和 HERG EP 的IC50值分别为 5 nM 和 34 μM。MK-8153 可用作利尿剂。

MK-8153 is a potent, selective and orally active inhibitor of renal outer medullary potassium channel (ROMK), with IC 50 s of 5 nM, 34 μM for ROMK electrophysiology (EP) and hERG EP, respectively. MK-8153 can be used as the diuretic/atriuretic [1].

MK-8153 inhibits current through rat ROMK, rKir1.1/HEK293 cells in electrophysiological recordings with an IC 50 of 2.5 nM [1].

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 [1]. 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) [1]. Animal Model: Aged spontaneously hypertensive rats (SHRs) [1] 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.

1548286-45-8

C24H28N2O6

440.49

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years