PF-8380 is an 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 (lysophosphatid
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of autotaxin
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
PF-8380 is a potent and specific autotaxin inhibitor with an IC50 value of 2.8 nM. A substrate competitive and tight-binding inhibitor of autotaxin.
Associated Targets(Human)
ENPP2TchemEctonucleotide pyrophosphatase/phosphodiesterase family member 2 (17 Activities)
1.Gierse J, Thorarensen A, Beltey K, Bradshaw-Pierce E, Cortes-Burgos L, Hall T, Johnston A, Murphy M, Nemirovskiy O, Ogawa S et al.. (2010) A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation.. J Pharmacol Exp Ther, 334 (1):(310-7). [PMID:20392816][10.1021/op500134e]
2.St-Cœur PD, Ferguson D, Morin Jr P, Touaibia M. (2013) PF-8380 and closely related analogs: synthesis and structure-activity relationship towards autotaxin inhibition and glioma cell viability.. Arch Pharm (Weinheim), 346 (2):(91-7). [PMID:23300119][10.1021/op500134e]
3.Castagna D, Budd DC, Macdonald SJ, Jamieson C, Watson AJ. (2016) Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature.. J Med Chem, 59 (12):(5604-21). [PMID:26745766][10.1021/op500134e]
Solution Calculators
Molarity Calculator
Determine the necessary mass, volume, or concentration for preparing a solution.
Dilution Calculator
Determine the dilution needed to prepare a stock solution.
H1616108