An inhibitor of autotaxin
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PF-8380

Item No. 12018

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[3-(2,3-dihydro-2-oxo-6-benzoxazolyl)-3-oxopropyl]-(3,5-dichlorophenyl)methyl ester-1-piperazinecarboxylic acid
CAS Number
1144035-53-9
Molecular Formula
C22H21Cl2N3O5
Formula Weight
478.3
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS(pH 7.2)(1:6): 0.14 mg/mlDMSO: 3 mg/ml
λmax
220, 273, 292 nm
SMILES
O=C(C1=CC(OC(N2)=O)=C2C=C1)CCN3CCN(C(OCC4=CC(Cl)=CC(Cl)=C4)=O)CC3
InChi Code
InChI=1S/C22H21Cl2N3O5/c23-16-9-14(10-17(24)12-16)13-31-22(30)27-7-5-26(6-8-27)4-3-19(28)15-1-2-18-20(11-15)32-21(29)25-18/h1-2,9-12H,3-8,13H2,(H,25,29)
InChi Key
JMSUDQYHPSNBSN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $53

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    5 mg

    $145

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    10 mg

    $186

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    25 mg

    $462

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    Product Description

    PF-8380 is a potent inhibitor of autotaxin (IC50 = 2.8 nM in an enzyme assay), the enzyme that converts lysophosphatidylcholine to lysophosphatidic acid (LPA).1 It reverses MMP-13 expression induced by leptin in human OA chondrocytes when used at a concentration of 10 µM.2 PF-8380 (30 mg/kg) reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gierse, J., Thorarensen, A., Beltey, K., et al. A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation. J. Pharmacol. Exp. Ther. 334(1), 310-317 (2010).

    2. Datta, P., Zhang, Y., Parousis, A., et al. High-fat diet-induced acceleration of osteoarthritis is associated with a distinct and sustained plasma metabolite signature. Sci. Rep. 7(1), 8205 (2017).

    Product Citations

    Datta, P., Zhang, Y., Parousis, A., et al. High-fat diet-induced acceleration of osteoarthritis is associated with a distinct and sustained plasma metabolite signature. Sci. Rep. 7(1), 8205 (2017).