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.
Product information
CAS Number: 1548286-45-8
Molecular Weight: 440.49
Formula: C24H28N2O6
Chemical Name: 8-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-1, 3-dihydro-2-benzofuran-5-yl)ethyl]-2-(4-methyl-5-oxo-2, 5-dihydrofuran-3-yl)-2, 8-diazaspiro[4.5]decan-1-one
Smiles: CC1=C(C=CC2=C1COC2=O)[C@@H](O)CN1CCC2(CCN(C3COC(=O)C=3C)C2=O)CC1
InChiKey: KDAIMYGCILCZSH-FQEVSTJZSA-N
InChi: InChI=1S/C24H28N2O6/c1-14-16(3-4-17-18(14)12-31-22(17)29)20(27)11-25-8-5-24(6-9-25)7-10-26(23(24)30)19-13-32-21(28)15(19)2/h3-4,20,27H,5-13H2,1-2H3/t20-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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).
Products are for research use only. Not for human use.
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