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ML297

Cat. No. M6975
ML297 Structure
Synonym:

VU 0456810; CID 56642816

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5mg USD 460 4-7 Days
10mg USD 770 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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 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

ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice
Kristian Kaufmann, et al. ACS Chem Neurosci. 2013 Sep 18;4(9):1278-86. PMID: 23730969.

Irreversible Nek2 kinase inhibitors with cellular activity.
Henise, et al. J Med Chem. 2011;54: 4133. PMID: 21627121.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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