189512 | Autotaxin Inhibitor III, PF-8380 - CAS 1144035-53-9 - Calbiochem

189512
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₂H₂₁Cl₂N₃O₅ 1144035-53-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      189512-10MG
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          Glass bottle 10 mg
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          Description
          OverviewAn orally bioavailable piperazinylbenzoxazolone compound that acts as a substrate competitive and tight-binding inhibitor of autotaxin activity {IC50 = 2.8 and 1.7 nM for recombinant human enzyme-β isoform employing FS-3 and LPC (lysophosphatidylcholine) as substrates, respectively; 1.16 and 1.15 nM for rat/murine enzyme-FS-3 and fetal fibroblast cell-LPC; 101 nM for human whole blood}. Displays desirable pharmacokinetics properties and efficiently blocks inflammation-induced LPA (lysophosphatidic acid) production both in plasma and at the site of inflammation by 95% in rat adjuvant-induced arthritis model (30 mg/kg, p.o.).
          Catalogue Number189512
          Brand Family Calbiochem®
          Synonyms6-(3-(Piperazin-1-yl)propanoyl)-benzo[d]oxazol-2(3H)-one, Atx Inhibitor III, PF-8380
          References
          ReferencesGierse, J., et al. 2010. J. Pharmacol. Exp. Ther. 334, 310.
          Product Information
          CAS number1144035-53-9
          FormTan powder
          Hill FormulaC₂₂H₂₁Cl₂N₃O₅
          Chemical formulaC₂₂H₂₁Cl₂N₃O₅
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥95% 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 Dry Ice Only
          Toxicity Standard Handling
          Storage -20°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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          189512

          References

          Reference overview
          Gierse, J., et al. 2010. J. Pharmacol. Exp. Ther. 334, 310.
          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.

          Revision17-August-2012 JSW
          Synonyms6-(3-(Piperazin-1-yl)propanoyl)-benzo[d]oxazol-2(3H)-one, Atx Inhibitor III, PF-8380
          DescriptionAn orally bioavailable piperazinylbenzoxazolone compound that acts as a substrate competitive and tight-binding inhibitor of autotaxin activity {IC50 = 2.8 and 1.7 nM for recombinant human enzyme-β isoform employing FS-3 and LPC (lysophosphatidylcholine) as substrates, respectively; 1.16 and 1.15 nM for rat/murine enzyme-FS-3 and fetal fibroblast cell-LPC; 101 nM for human whole blood}. Displays desirable pharmacokinetics properties and efficiently blocks inflammation-induced LPA (lysophosphatidic acid) production both in plasma and at the site of inflammation by 95% in rat adjuvant-induced arthritis model (30 mg/kg, p.o.).
          FormTan powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1144035-53-9
          Chemical formulaC₂₂H₂₁Cl₂N₃O₅
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage -20°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
          ReferencesGierse, J., et al. 2010. J. Pharmacol. Exp. Ther. 334, 310.