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ML297

Cat. No. M6975
ML297 Structure
Synonym:

VU 0456810; CID 56642816

Size Price Availability
5mg USD 460  USD460 4-7 Days
10mg USD 770  USD770 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

ML297 is a selective Kir3.1/3.2 (GIRK1/2) channel activator (IC50 values are 160, 887 and 914 nM for GIRK1/2, GIRK1/4 and GIRK1/3 respectively). ML297 exhibits no effect on GIRK2, GIRK2/3, Kir2.1 and Kv7.4 channels, and has minimal effect on a panel of other ion channels, receptors and transporters. ML297 prevents PTZ-induced epileptic seizures in mice. Brain penetrant.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 328.32
Formula C17H14F2N4O
CAS Number 1443246-62-5
Purity >98%
Solubility DMSO ≥ 20 mg/mL
Storage at -20°C
References

[1] Kristian Kaufmann, et al. ACS Chem Neurosci. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice

[2] Henise, et al. J Med Chem. Irreversible Nek2 kinase inhibitors with cellular activity.

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  Catalog
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Keywords: ML297, VU 0456810; CID 56642816 supplier, Potassium Channel, inhibitors

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