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VU0134992 

Cat. No. M30578
VU0134992  Structure
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Quality Control & Documentation
Biological Activity

VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.

Chemical Information
Molecular Weight 411.38
Formula C20H31BrN2O2
CAS Number 755002-90-5
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] Yun-Hao Jiang, et al. Glia. Contribution of inwardly rectifying K+ channel 4.1 of supraoptic astrocytes to the regulation of vasopressin neuronal activity by hypotonicity

[2] Jing Lu, et al. Cell Mol Life Sci. Inwardly rectifying potassium channels mediate polymyxin-induced nephrotoxicity

[3] Elena Isaeva, et al. Br J Pharmacol. Crosstalk between epithelial sodium channels (ENaC) and basolateral potassium channels (Kir 4.1/Kir 5.1) in the cortical collecting duct

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

[5] Sujay V Kharade, et al. Mol Pharmacol. Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992

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  Catalog
Abmole Inhibitor Catalog




Keywords: VU0134992  supplier, Potassium Channel, inhibitors, activators


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