217384
GIRK Activator, ML297 (1-(3,4-Difluorophenyl)-3-(3-methyl-1-phenyl-1H-pyrazol-5-yl)urea, N-(3,4-Difluorophenyl)-N′-(3-methyl-1-phenyl-1H-pyrazol-5-yl)urea, CID 56642816, VU0456810)
Size
£451.00
- SKU:
- 217384
- Purity:
- ≥98% (HPLC)
- Storage Conditions:
- 4°C
- Supplier:
- United States Biological
- CAS Number:
- 1443246-62-5
- Format:
- White powder.
- Extra Details:
- A blood-brain barrier-permeable, non-toxic phenyl-pyrazolylurea compound that acts as a direct, potent, fast, and reversible activator of GIRK1 (G-protein activated inward-rectifying K+ channel containing subunit 1) containing channels (EC50 = 162, 914, and 887nM in Thallium influx assay for GIRK1/2, GIRK1/3, and GIRK1/4 expressed in HEK-293 cell lines). Its action does not require the presence of an activated Gi GPCR. Shown to be inactive towards GIRK2, GIRK2/3, Kir2.1, KV7.4 and GABAA, and weakly active against a panel of 61 other receptors, ion channels, enzymes, transporters, and proteins even at higher concentration (~10uM). Exhibits desirable pharmacokinetic properties with good solubility (17.5uM), predicted hepatic clearance (88 ml/min/kg), and Tmax of 640nM and 130nM in plasma and brain, respectively. Shown to reduce locomotor function and seizure frequency in electroshock- and chemically-induced murine epilepsy models (60mg/kg, i.p). Synonyms: CID 56642816, VU0456810, 1-(3,4-Difluorophenyl)-3-(3-methyl-1-phenyl-1H-pyrazol-5-yl)urea, N-(3,4-Difluorophenyl)-Nʹ-(3-methyl-1-phenyl-1H-pyrazol-5-yl)urea CAS No: 1443246-62-5 Molecular Formula: C₁₇H₁₄F₂N₄O Solubility: DMSO Primary Target: GIRK1/Kir3.1-containing tetrameric GIRK channels Purity: ≥98% (HPLC) Appearance: White powder. Storage and Stability: May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
- Shipping Conditions:
- Blue Ice