ML297

SKU: orb1222696

Description

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.

Key Properties

• CAS Number: 1443246-62-5
• MW: 328.11
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₄F₂N₄O
• SMILES: Fc1ccc(cc1F)NC(=O)Nc3cc(C)nn3c2ccccc2
• Target: GIRK1/2
• Solubility: In Vitro: DMSO : 250 mg/mL (761.45 mM)

Bioactivity

• In Vivo:
  ML297 (60 mg/kg; i.p.) shows a highly significant ability to both prevent convulsions and prevent fatality of the PTZ treatment. Animal model: 8-10 months old C57/BL6 male mice (approximately 30 g). Dosage: 60 mg/kg. Administration: Intraperitoneal injection. Result: Most of the animals neither convulsions nor death.
• In Vitro:
  ML 297 is completely inactive for GIRK2/3.ML297 shows concentration-dependent efficacy in expressing GIRK1/2 cells and with an EC50 of 162 nM. ML297 shows a complete inability to modulate the activity of HEK-293 cells expressing GIRK2 alone and GIRKGIRK2/3.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ML297 | ML 297 | ML-297

Quick Database Links

Gene Symbol

GIRK1/2