MK-8153
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.
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- No. CAS: 1548286-45-8
- Fòrmula: C24H28N2O6
- Peso molecular:440.49
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
IC50: 5 nM (ROMK EP), 34 μM (hERG EP)[1]
MK-8153 inhibits current through rat ROMK, rKir1.1/HEK293 cells in electrophysiological recordings with an IC50 of 2.5 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Aged spontaneously hypertensive rats (SHRs)[1]
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Dosage:0.1, 0.3, 1, 3, 10 mg/kg
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Administration:P.o. once daily for 3 days
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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.
Chemical Information
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No. CAS 1548286-45-8
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Peso molecular 440.49
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Fòrmula C24H28N2O6
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SMILES
O=C1N(C2=C(C)C(OC2)=O)CCC13CCN(C[C@@H](C4=C(C)C5=C(C(OC5)=O)C=C4)O)CC3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MK-8153 Related Classifications
HY-132201 Related Classifications
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