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500486 CXCR3 Antagonist - Calbiochem

500486
  
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₂H₁₆F₂N6O₂S
      Description
      OverviewAn arylsulfonamide derivative that acts as a CXCR3 antagonist (IC50 = 192 nM against CXCL10-induced chemotaxis of hCXCR3-overexpressing L1.2 cells) with good aqueous solubility (>100 µM at pH 7.4). Shown to be orally available in mice (83% bioavailability; t1/2 = 1 h; 10 mg/kg p.o.) in vivo and display a medium intrinsic clearance (CIint = 17 µL/min/mg) in in vitro mouse liver microsome stability test.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number500486
      Brand Family Calbiochem®
      SynonymsGPR9 Antagonist, 4-cyano-N-(3-fluoro-4-(1H-tetrazol-5-yl)benzyl)-N-(2-fluorobenzyl)benzenesulfonamide, AS612568, EMD1205395, CD183 Antagonist
      References
      ReferencesCrosignani, S., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3614.
      Product Information
      FormYellow solid
      Hill FormulaC₂₂H₁₆F₂N6O₂S
      Chemical formulaC₂₂H₁₆F₂N6O₂S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCXCR3
      Primary Target IC<sub>50</sub>192 nM
      Purity≥95% 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 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
      Catalog Number GTIN
      500486 0

      Documentation

      CXCR3 Antagonist - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Crosignani, S., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3614.
      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.

      Revision21-November-2014 JSW
      SynonymsGPR9 Antagonist, 4-cyano-N-(3-fluoro-4-(1H-tetrazol-5-yl)benzyl)-N-(2-fluorobenzyl)benzenesulfonamide, AS612568, EMD1205395, CD183 Antagonist
      DescriptionAn arylsulfonamide derivative that acts as a CXCR3 antagonist (IC50 = 192 nM against CXCL10-induced chemotaxis of hCXCR3-overexpressing L1.2 cells) with good aqueous solubility (>100 µM at pH 7.4). Shown to be orally available in mice (83% bioavailability; t1/2 = 1 h; 10 mg/kg p.o.) in vivo and display a medium intrinsic clearance (CIint = 17 µL/min/mg) in in vitro mouse liver microsome stability test.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₂H₁₆F₂N6O₂S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 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
      ReferencesCrosignani, S., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3614.