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506045 GPR55 Receptor Antagonist, CID16020046 - CAS 834903-43-4 - Calbiochem

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Synonymes: 4-[4-(3-Hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1H,4H-pyrrolo[3,4-c]pyrazol-5-yl]benzoic Acid

Primary Target: GPR55
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506045
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Tableau de caractéristiques principal

CAS #Empirical Formula
834903-43-4C₂₅H₁₉N₃O₄

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      Description
      OverviewA selective antagonist of G protein-coupled receptor 55 (GPR55) that blocks lipid L-a-lysophosphatidylinositol (LPI, Cat. No. 440153)-induced GPR55 activation (IC50 = 1 µM) and downstream effects in HEK293 cells. Also shown to block the agonistic effect of LPI on GPR55- expressing yeast cells (~10 µM). Inhibits LPI-induced Ca2+ mobilization and ERK1/2 phosphorylation in HEK-GPR55 and HEK-CB1 cells. However, it does not affect basal Ca2+ mobilization and ERK1/2 activity. Blocks the GPR55-mediated NFAT and NF-kB activation and their nuclear translocation in HEK-GPR55 cells. Diminishes LPI-induced wound healing in GPR55-expressing primary human lung microvascular endothelial cells and reverses LPI-inhibited platelet aggregation (~10 µM). Also reported to inhibit the activity of phosphodiesterases PDE3A and PDE4B (pIC50 = 5 and 4.8, respectively).
      Catalogue Number506045
      Brand Family Calbiochem®
      Synonyms4-[4-(3-Hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1H,4H-pyrrolo[3,4-c]pyrazol-5-yl]benzoic Acid
      References
      ReferencesKargl, J., et al, 2013. J. Pharmacol. Exp. Ther. 346, 54.
      Product Information
      CAS number834903-43-4
      FormOff-white powder
      Hill FormulaC₂₅H₁₉N₃O₄
      Chemical formulaC₂₅H₁₉N₃O₄
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetGPR55
      Primary Target IC<sub>50</sub>1 µ
      Purity≥99% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5.06045.0001 04055977262674

      Documentation

      GPR55 Receptor Antagonist, CID16020046 - CAS 834903-43-4 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Kargl, J., et al, 2013. J. Pharmacol. Exp. Ther. 346, 54.
      Fiche technique

      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
      Synonyms4-[4-(3-Hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1H,4H-pyrrolo[3,4-c]pyrazol-5-yl]benzoic Acid
      DescriptionA selective antagonist of G protein-coupled receptor 55 (GPR55) that blocks lipid L-a-lysophosphatidylinositol (LPI, Cat. No. 440153)-induced GPR55 activation (IC50 = 1 µM) and downstream effects in HEK293 cells. Also shown to block the agonistic effect of LPI on GPR55- expressing yeast cells (~10 µM). Inhibits LPI-induced Ca2+ mobilization and ERK1/2 phosphorylation in HEK-GPR55 and HEK-CB1 cells. However, it does not affect basal Ca2+ mobilization and ERK1/2 activity. Blocks the GPR55-mediated NFAT and NF-kB activation and their nuclear translocation in HEK-GPR55 cells. Diminishes LPI-induced wound healing in GPR55-expressing primary human lung microvascular endothelial cells and reverses LPI-inhibited platelet aggregation (~10 µM). Also reported to inhibit the activity of phosphodiesterases PDE3A and PDE4B (pIC50 = 5 and 4.8, respectively).
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number834903-43-4
      Chemical formulaC₂₅H₁₉N₃O₄
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesKargl, J., et al, 2013. J. Pharmacol. Exp. Ther. 346, 54.