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

The Autotaxin Inhibitor III, PF-8380, also referenced under CAS 1144035-53-9, controls the biological activity of Autotaxin. This small molecule/inhibitor is primarily used for Membrane applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 6-(3-(Piperazin-1-yl)propanoyl)-benzo[d]oxazol-2(3H)-one, Atx Inhibitor III, PF-8380

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189512
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1144035-53-9C₂₂H₂₁Cl₂N₃O₅

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189512-10MG
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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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalogue Number GTIN
      189512-10MG 04055977221886

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      Autotaxin Inhibitor III, PF-8380 - CAS 1144035-53-9 - Calbiochem 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 Protect from light
      -20°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 Standard Handling
      ReferencesGierse, J., et al. 2010. J. Pharmacol. Exp. Ther. 334, 310.