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PF-8380

Catalog No: 17030115
CAS Number: 1144035-53-9
Purity: 98% 

PF-8380 is a potent autotaxin inhibitor with an IC(50) of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood. PF-8380 has adequate oral bioavailability and exposures required for in vivo testing of autotaxin inhibition. Autotaxin's role in producing LPA in plasma and at the site of inflammation was tested in a rat air pouch model. The specific inhibitor PF-8380 , dosed orally at 30 mg/kg, provided >95% reduction in both plasma and air pouch LPA within 3 h, indicating autotaxin is a major source of LPA during inflammation. At 30 mg/kg PF-8380 reduced inflammatory hyperalgesia with the same efficacy as 30 mg/kg naproxen. 

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Chemical Information

NamePF-8380
Iupac Chemical NamePF-8380 
SynonymsPF8380; PF-8380; PF 8380 
Molecular FormulaC22H21Cl2N3O5 
Molecular Weight478.32 
Smilec1cc2c(cc1C(=O)CCN3CCN(CC3)C(=O)OCc4cc(cc(c4)Cl)Cl)oc(=O)[nH]2
InChiKeyJMSUDQYHPSNBSN-UHFFFAOYSA-N
InChiInChI=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)
CAS Number1144035-53-9
MDLMFCD20527274
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Ordering Information

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Formulationoff-white solid 
Purity98% 
Storage3 years -20ºCpowder 
SolubilitySoluble in DMSO 
Handling
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
HS Code
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study
Not available

Chemical Structure

17030115 - PF-8380 | CAS 1144035-53-9

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