MK-8153 |
| Katalog-Nr.GC70656 |
MK-8153 ist ein potenter, selektiver und oral aktiver Inhibitor des renalen äußeren medullaren Kaliumkanals (ROMK), mit IC50s von 5 nM, 34 μM für ROMK Elektrophysiologie (EP) bzw. hERG EP.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1548286-45-8
Sample solution is provided at 25 µL, 10mM.
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MK-8153 inhibits current through rat ROMK, rKir1.1/HEK293 cells in electrophysiological recordings with an IC50 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].
References:
[1]. Jiang J, et, al. Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic. J Med Chem. 2021 May 26.
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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