MK-8153,1548286-45-8

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MK-8153

CAS No. : 1548286-45-8

MCE 国际站：MK-8153

产品活性：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。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

In Vitro: MK-8153 inhibits current through rat ROMK, rKir1.1/HEK293 cells in electrophysiological recordings with an IC₅₀ of 2.5 nM.

In Vivo: 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).

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