1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. MK-8153

MK-8153 

Cat. No.: HY-132201
Handling Instructions

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.

For research use only. We do not sell to patients.

MK-8153 Chemical Structure

MK-8153 Chemical Structure

CAS No. : 1548286-45-8

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Description

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[1].

IC50 & Target

IC50: 5 nM (ROMK EP), 34 μM (hERG EP)[1]

In Vitro

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

440.49

Formula

C₂₄H₂₈N₂O₆

CAS No.
SMILES

O=C1N(C2=C(C)C(OC2)=O)CCC13CCN(C[[email protected]@H](C4=C(C)C5=C(C(OC5)=O)C=C4)O)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

MK-8153MK8153MK 8153Potassium ChannelKcsArenaloutermedullarypotassiumchannelROMKelectrophysiologyEPhERGdiureticatriureticInhibitorinhibitorinhibit

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