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189511 Autotaxin Inhibitor II, HA130 - Calbiochem

189511
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₄H₁₉BFNO₅S

Products

Catalogue NumberPackaging Qty/Pack
189511-10MG Glass bottle 10 mg
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 SDS

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.