PF 8380

Tocris Bioscience | Catalog # 4078

Potent autotaxin inhibitor
Tocris Bioscience
Discontinued Product
4078 has been discontinued. View all Autotaxin Inhibitors products.

Key Product Details

Description

Potent autotaxin inhibitor
View all Autotaxin Inhibitors »

Product Description

PF 8380 is a potent autotaxin inhibitor (IC50 = 2.8 nM in isolated enzyme assay; 101 nM in human whole blood). Modulates lysophosphatidic acid (LPA) levels in vivo and in vitro by directly inhibiting autotaxin; reduces LPA levels both in plasma and at site of inflammation. Decreases leptin-induced MMP13 expression, in vitro. Orally available.

Product Specifications for PF 8380

Molecular Weight

478.33

Formula

C22H21Cl2N3O5

Storage

Store at -20°C

Purity

≥97% (HPLC)

Chemical Name

3,5-Dichlorobenzyl-[4-[3-oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]]piperazine-1-carboxylate

CAS Number

1144035-53-9

PubChem ID

25265312

InChI Key

JMSUDQYHPSNBSN-UHFFFAOYSA-N

SMILES

O=C(C2=CC(OC(N4)=O)=C4C=C2)CCN1CCN(C(OCC3=CC(Cl)=CC(Cl)=C3)=O)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 47.83 100

Preparing Stock Solutions for PF 8380

The following data is based on the product molecular weight 478.33.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.09 mL 10.45 mL 20.91 mL
5 mM 0.42 mL 2.09 mL 4.18 mL
10 mM 0.21 mL 1.05 mL 2.09 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Background References

References are publications that support the biological activity of the product.

Product Documents for PF 8380

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for PF 8380

For research use only

Customer Reviews for PF 8380 (2)

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  • The effect of ATX inhibition on LPS induced pro-inflammatory phenotype in microglia.
    Name: lisha joshi
    Species: Mouse
    Assay Type: In Vitro
    Cell Line/Tissue: BV2 microglia cells
    Verified Customer | Posted 06/10/2019
    PF8380 was used to inhibit autotaxin in BV2 microglia cells in order to study the effect of ATX-LPA axis on microglia proinflammatory phenotype. Cells were treated with LPS (20ng/mi) in the absence or presence of the inhibitor (10µM) for 24 hours and then collected for RNA isolation and subsequent analysis of iNOS and TNFa expression with qPCR.
    PF 8380 4078
  • PF 8380 decreases the levels of lysophosphatidic acid in mouse brain
    Name: Joanna Plastira
    Species: Mouse
    Assay Type: In Vivo
    Cell Line/Tissue: Brain
    Verified Customer | Posted 10/10/2018
    During preliminary studies we investigated whether the ATX inhibitor PF-8380 crosses the BBB and impacts LPA levels in the brain. After oral gavage of 3mg/kg PF-8380 per mouse (PF-8380 was dissolved in hydroxyl methyl cellulose), mice were anesthetized and perfused with PBS at different time points and the whole brains were dissected and immediately snap frozen in liquid nitrogen. Lipids were extracted using the Bligh & Dyer HCl method and the levels of LPA and PF-8380 were quantitated by LC-MS/MS.
    PF 8380 4078

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