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505820 GIRK Activator, ML297 - CAS 1443246-62-5 - Calbiochem

505820
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Empirical FormulaCAS #
C₁₇H₁₄F₂N₄O 1443246-62-5

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      Description
      OverviewA 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 887 nM 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 (~10 µM). Exhibits desirable pharmacokinetic properties with good solubility (17.5 µM), predicted hepatic clearance (88 ml/min/kg), and Tmax of 640 nM and 130 nM in plasma and brain, respectively. Shown to reduce locomotor function and seizure frequency in electroshock- and chemically-induced murine epilepsy models (60 mg/kg, i.p).
      Catalogue Number505820
      Brand Family Calbiochem®
      SynonymsCID 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
      References
      ReferencesWen, W., et al. 2013. Bioorg. Med. Chem. Lett. 23, 4562.
      Kaufmann, K., et al. 2013. ACS Chem. Neurosci. 4, 1278.
      Product Information
      CAS number1443246-62-5
      FormWhite powder
      Hill FormulaC₁₇H₁₄F₂N₄O
      Chemical formulaC₁₇H₁₄F₂N₄O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetGIRK1/Kir3.1-containing tetrameric GIRK channels
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      GIRK Activator, ML297 - CAS 1443246-62-5 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Wen, W., et al. 2013. Bioorg. Med. Chem. Lett. 23, 4562.
      Kaufmann, K., et al. 2013. ACS Chem. Neurosci. 4, 1278.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision18-October-2013 JSW
      SynonymsCID 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
      DescriptionA cell-permeable phenyl-pyrazolylurea that directly activates GIRK1/Kir3.1-containing tetrameric GIRK channels (EC50 = 162, 887 and 914 nM, respectively, in Thallium flux assays using GIRK1-2, GIRK1-4, or GIRK1-3 HEK-293 transfectants; EC50 = 584 and 1,400 nM, respectively, in whole-cell voltage clamp measurements using GIRK1-2 or GIRK1-4 HEK-293 transfectants) in a GPCR-independent manner, while being ineffective toward Kir2.1, KV7.4, or GIRK channels composed of GIRK2-3 (Kir3.2-Kir3.3) or GIRK2 alone. Selectivity studies against 67 receptors reveal only weak antagonistic activity against hERG (IC50 = 10 µM; Inhmax/ICmax = 59.6%/100 µM), rat GABAA (muscimol), human Sigma δ1, and human 5-HT2B receptors (49%, 49%, and 46% inhibition, respectively, at 10 µM). Despite its suboptimal metabolic stability and brain permeability in mice (Cmax/Tmaxmax = 130 nM/30 min; 60 mg/kg i.p.), ML297 nevertheless is demonstrated to be at least 4.9-times more effective than Valproate (Cat. No. 676380) in prolonging the latency to seizure following lethal electric shock and in preventing GABAA antagonist PTZ-induced convulsion and death in two murine epilepsy models (60 mg/kg i.p.) in vivo.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1443246-62-5
      Chemical formulaC₁₇H₁₄F₂N₄O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesWen, W., et al. 2013. Bioorg. Med. Chem. Lett. 23, 4562.
      Kaufmann, K., et al. 2013. ACS Chem. Neurosci. 4, 1278.