189511 Autotaxin Inhibitor II, HA130 - Calbiochem

189511
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₄H₁₉BFNO₅S

Pricing & Availability

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189511-10MG
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      Description
      OverviewA thiazolidinedione that is designed to target the ATX active site thr210 with a boronic moiety and shown to potently inhibit ATX lysoPLD activity (IC50 ~28 nM using recombinant human ATX or human plasma) in a reversible manner with a mixed-type Lineweaver-Burk kinetics. Reported to exhibit low cytotoxicity (TD50 = 83, 105, and 2056 µM in HEK293T, A2058, and HepG2 cultures) and no activity toward NPP1, PDE, AP, or proteasomal chymotryptic/tryptic/caspase-like activities even at concentrations as high as 10 µM. Although HA130 quickly and effectively reduces circulating LPA level when injected in mice (463 µg/kg, i.v.) in vivo, the effect appears short-lived as is the case with S32826 (Cat. No. 189510).
      Catalogue Number189511
      Brand Family Calbiochem®
      SynonymsATX Inhibitor II, (Z)-3-((4-((3-(4-Fluorobenzyl)-2,4-dioxo-1,3-thiazolan-5-yliden)-methyl)phenoxy)methyl)benzeneboronic acid
      References
      ReferencesAlbers, H.M.H.G. et al. 2010. J. Med. Chem. 53, 4958.
      Albers, H.M.H.G. et al. 2010. Proc. Natl. Acad. Sci. USA 107, 7257.
      Product Information
      FormOff-white solid
      Hill FormulaC₂₄H₁₉BFNO₅S
      Chemical formulaC₂₄H₁₉BFNO₅S
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% 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 Regulatory Review
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      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

      Autotaxin Inhibitor II, HA130 - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      Autotaxin Inhibitor II, HA130 - Calbiochem Certificates of Analysis

      TitleLot Number
      189511

      References

      Reference overview
      Albers, H.M.H.G. et al. 2010. J. Med. Chem. 53, 4958.
      Albers, H.M.H.G. et al. 2010. Proc. Natl. Acad. Sci. USA 107, 7257.
      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.

      Revision31-March-2011 RFH
      SynonymsATX Inhibitor II, (Z)-3-((4-((3-(4-Fluorobenzyl)-2,4-dioxo-1,3-thiazolan-5-yliden)-methyl)phenoxy)methyl)benzeneboronic acid
      DescriptionA thiazolidinedione that is designed to target the ATX active site thr210 with a boronic moiety and shown to potently inhibit ATX lysoPLD activity (IC50 ~28 nM using recombinant human ATX or human plasma) in a reversible manner with a mixed-type Lineweaver-Burk kinetics. Reported to exhibit low cytotoxicity (TD50 = 83, 105, and 2056 µM in HEK293T, A2058, and HepG2 cultures) and no activity toward NPP1, PDE, AP, or proteasomal chymotryptic/tryptic/caspase-like activities even at concentrations as high as 10 µM. Although HA130 quickly and effectively reduces circulating LPA level when injected in mice (463 µg/kg, i.v.) in vivo, the effect appears short-lived as is the case with S32826 (Cat. No.189510).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₄H₁₉BFNO₅S
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage -20°C
      Hygroscopic
      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 Regulatory Review
      ReferencesAlbers, H.M.H.G. et al. 2010. J. Med. Chem. 53, 4958.
      Albers, H.M.H.G. et al. 2010. Proc. Natl. Acad. Sci. USA 107, 7257.