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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 Specifications Table

CAS #Empirical Formula
1144035-53-9C₂₂H₂₁Cl₂N₃O₅

Products

Catalog NumberPackaging Qty/Pack
189512-10MG Glass bottle 10 mg
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
Catalog 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.