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ML418 

Cat. No. M29031
ML418  Structure
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Biological Activity

ML418 is a potent, selective and CNS penetrating Kir7.1 potassium channel blocker. ML418 inhibits Kir7.1 with an IC50 value of 0.31 μM. ML418 can be used for the research of neurological, cardiovascular, endocrine and muscle disorders.

Chemical Information
Molecular Weight 377.87
Formula C19H24ClN3O3
CAS Number 1928763-08-9
Form Solid
Solubility (25°C) DMSO 20.83 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] You-You Lv, et al. CNS Neurosci Ther. SUMOylation of Kir7.1 participates in neuropathic pain through regulating its membrane expression in spinal cord neurons

[2] C David Weaver, et al. Am J Physiol Cell Physiol. Next-generation inward rectifier potassium channel modulators: discovery and molecular pharmacology

[3] David Ermert, et al. Mol Immunol. The hijackers guide to escaping complement: Lessons learned from pathogens

[4] Sujay V Kharade, et al. Mol Pharmacol. Pore Polarity and Charge Determine Differential Block of Kir1.1 and Kir7.1 Potassium Channels by Small-Molecule Inhibitor VU590

[5] Daniel R Swale, et al. ACS Chem Neurosci. ML418: The First Selective, Sub-Micromolar Pore Blocker of Kir7.1 Potassium Channels

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Keywords: ML418  supplier, Potassium Channel, inhibitors, activators


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