ML365

SKU: orb1221638

Description

ML365 is a potent and selective K2P3.1 TASK-1 channel blocker. ML365 blocks TASK1 channels in both the thallium influx fluorescent assay (IC50 = 4 nM) and an automated electrophysiology assay (IC50 = 16 nM). Based on potency differences, it possesses more than 60-fold selectivity for inhibition of TASK1 over a closely-related, two-pore domain potassium channel, TASK3. ML365 displays little or no inhibition at 30 μM of more distantly related potassium channels, Kir2.1, potassium voltage-gated channel, KQT-like subfamily, member 2 (KCNQ2), and human ether-a go-go-related gene (hERG). Based on these criteria, ML365 is a best-in-class probe and is a useful pharmacological probe for in vitro studies of TASK1 function and in further studies aimed at developing therapeutic intervention.

Key Properties

• CAS Number: 947914-18-3
• MW: 360.41
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₀N₂O₃
• SMILES: COc1ccccc1C(=O)Nc1cccc(NC(=O)c2cccc(C)c2)c1
• Target: CDK
• Solubility: DMSO : ≥ 100 mg/mL 277.46 mM H2O : < 0.1 mg/mL

Bioactivity

• In Vitro:
  ML365 blocks TASK1 channels in both the thallium influx fluorescent assay (IC50 = 4 nM) and an automated electrophysiology assay (IC50 = 16 nM). ML365 displays little or no inhibition at 30 μM of more distantly related potassium channels, Kir2.1, potassium voltage-gated channel, KQT-like subfamily, member 2 (KCNQ2), and human ether-a go-go-related gene (hERG). ML365 does not exhibit acute toxicity in cell-based assays at concentrations up to 30 μM.

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

ML365 | ML-365 | ML 365

Quick Database Links

Gene Symbol

CDK