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MK-7145 

Cat. No. M28056
MK-7145  Structure
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Quality Control & Documentation
Biological Activity

MK-7145 is a ROMK inhibitor, with an IC50 of 0.045 μM.

Chemical Information
Molecular Weight 466.53
Formula C26H30N2O6
CAS Number 1255204-84-2
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jinlong Jiang, et al. J Med Chem. Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic

[2] Birgit T Priest, et al. Future Med Chem. The therapeutic potential of targeting the Kir1.1 (renal outer medullary K+) channel

[3] Vincenzo Calderone, et al. Curr Med Chem. The Renal Outer Medullary Potassium Channel (ROMK): An Intriguing Pharmacological Target for an Innovative Class of Diuretic Drugs

[4] Haifeng Tang, et al. ACS Med Chem Lett. Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure

[5] Caryn Hampton, et al. J Pharmacol Exp Ther. The Renal Outer Medullary Potassium Channel Inhibitor, MK-7145, Lowers Blood Pressure, and Manifests Features of Bartter's Syndrome Type II Phenotype

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Keywords: MK-7145  supplier, Potassium Channel, inhibitors, activators


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