Free shipping on all orders over $ 500

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
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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.

Chemical Information
Molecular Weight 328.32
Formula C17H14F2N4O
CAS Number 1443246-62-5
Solubility (25°C) DMSO ≥ 20 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] 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.

Related Potassium Channel Products
NPBA

NPBA is a potassium K2P channel TASK-3 (KCNK9) agonist and a tandem pore domain weak inward rectifier K+ channel (TWIK2) channel blocker. In addition, NPBA inhibits the activation of NLRP3 inflammasome in macrophages.

BeKm-1

BeKm-1 is a HERG (human ether-a-go-go-related gene) blocking compound.

Apamin

Apamin (Apamine) is a specifically selective blocker of Ca2+-activated K+ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.

Phe-Met-Arg-Phe amide trifluoroacetate

Phe-Met-Arg-Phe amide trifluoroacetate is an activator of K+ current, with ED50 of 23 nM in the peptidergic caudodorsal neurons.

Iberiotoxin

Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom.

  Catalog
Abmole Inhibitor Catalog




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


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.