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567736 S1P₂ Receptor Antagonist, JTE-013

567736
  
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      Overview

      Replacement Information
      Description
      OverviewA cell-permeable pyrazolopyridine compound that acts as a potent S1P2-selective S1P receptor antagonist (IC50 = 17 nM and 22 nM in CHO cells stably transfected with human S1P2 and rat S1P2, respectively; IC50 >10 µM for S1P1 and S1P3). Specifically blocks S1P binding to S1P2 and prevents S1P2-mediated intracellular Ca2+-mobilization and ERK activation, reverses the regulatory actions of S1P (Cat. No. 567727) on cell migration and invasion, cAMP accumulation and RANTES production.
      Catalogue Number567736
      Brand Family Calbiochem®
      Synonyms1-(1,3-Dimethyl-4-isopropyl)-1H-pyrazolo[3,4-b]pyridin-6-yl)-4-(3,5-dichloro-4-pyridinyl)-semicarbazide, JTE-013
      References
      ReferencesDamirin, A., et al. 2005. Mol. Pharmacol. 67, 1177. Kawata, T., et al. 2005. Biochem. Biophys. Res. Commun. 331, 640. Ikeda, H., et al. 2004. Biochem. Biophys. Res. Commun. 320, 754. Arikawa, K., et al. 2003. J. Biol. Chem. 278, 32841. Osada, M., et al. 2002. Biochem. Biophys. Res. Commun. 299, 483.
      Product Information
      CAS number547756-93-4
      FormPale-yellow solid
      Hill FormulaC₁₇H₁₉N₇OCl₂
      Chemical formulaC₁₇H₁₉N₇OCl₂
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      ImmunogenPlease do not archive or activate this record pending patent review. JSW 08-28-08
      Purity≥98% 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 Ambient Temperature Only
      Toxicity Irritant
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      567736 0

      Documentation

      S1P₂ Receptor Antagonist, JTE-013 Certificates of Analysis

      TitleLot Number
      567736

      References

      Reference overview
      Damirin, A., et al. 2005. Mol. Pharmacol. 67, 1177. Kawata, T., et al. 2005. Biochem. Biophys. Res. Commun. 331, 640. Ikeda, H., et al. 2004. Biochem. Biophys. Res. Commun. 320, 754. Arikawa, K., et al. 2003. J. Biol. Chem. 278, 32841. Osada, M., et al. 2002. Biochem. Biophys. Res. Commun. 299, 483.
      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.

      Revision11-September-2008 RFH
      Synonyms1-(1,3-Dimethyl-4-isopropyl)-1H-pyrazolo[3,4-b]pyridin-6-yl)-4-(3,5-dichloro-4-pyridinyl)-semicarbazide, JTE-013
      DescriptionA cell-permeable pyrazolopyridine compound that acts as a potent S1P2-selective S1P receptor antagonist (IC50 = 17 nM and 22 nM in CHO cells stably transfected with human S1P2 and rat S1P2, respectively; IC50 >10 µM for S1P1 and S1P3). Specifically blocks S1P binding to S1P2 and prevents S1P2-mediated intracellular Ca2+-mobilization and ERK activation, reverses the regulatory actions of S1P (Cat. No. 567727) on cell migration and invasion, cAMP accumulation and RANTES production.
      ImmunogenPlease do not archive or activate this record pending patent review. JSW 08-28-08
      FormPale-yellow solid
      CAS number547756-93-4
      Chemical formulaC₁₇H₁₉N₇OCl₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (40 mg/ml) or Ethanol (40 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 6 months at -20°C.
      Toxicity Irritant
      ReferencesDamirin, A., et al. 2005. Mol. Pharmacol. 67, 1177. Kawata, T., et al. 2005. Biochem. Biophys. Res. Commun. 331, 640. Ikeda, H., et al. 2004. Biochem. Biophys. Res. Commun. 320, 754. Arikawa, K., et al. 2003. J. Biol. Chem. 278, 32841. Osada, M., et al. 2002. Biochem. Biophys. Res. Commun. 299, 483.