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Cat. No.: HY-132201

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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.

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

CAS No.: 1548286-45-8
Formula: C₂₄H₂₈N₂O₆
Molecular Weight:440.49

Storage:

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

Data Sheet (274 KB)

MK-8153 Chemical Structure

CAS No.: 1548286-45-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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].

MedChemExpress (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].

MedChemExpress (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.

Chemical Information

CAS No. 1548286-45-8
Molecular Weight 440.49
Formula C₂₄H₂₈N₂O₆
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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