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VU591

Cat. No. M8223
VU591 Structure
Size Price Availability
10mg USD 150  USD150 4-7 Days
50mg USD 560  USD560 4-7 Days
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Quality Control & Documentation
Biological Activity

VU591 is a Potassium Inwardly-Rectifying Channel (KCNJ1 or ROMK) specific inhibitor (IC50 = 240 nM) that is closely related to VU590. Unlike VU590, VU591 does not inhibit Kir7.1. The compound has a modest effect on Kir6.2/SUR1, causing 17% inhibition at 10 uM.

Chemical Information
Molecular Weight 368.3
Formula C16H12N6O5
CAS Number 1222810-74-3
Form Solid
Solubility (25°C) DMSO: ≥12 mg/mL
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] Gautam Bhave, et al. Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel

[2] Daniel R Swale, et al. Computational and functional analyses of a small-molecule binding site in ROMK

[3] Jiun-Lin Horng, et al. Potassium Regulation in Medaka (Oryzias latipes) Larvae Acclimated to Fresh Water: Passive Uptake and Active Secretion by the Skin Cells

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