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Autotaxin converts lysophosphatidylcholine to lysophosphatidic acid (LPA), which can mediate changes in cell proliferation, angiogenesis, and cytokine secretion.{21340} 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).{21340} It reverses MMP-13 expression induced by leptin in human OA chondrocytes when used at a concentration of 10 µM.{35249} 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).{21340}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 25 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1144035-53-9 |
| Molecular formula | C22H21Cl2N3O5 |
| Smiles | O=C(C1=CC(OC(N2)=O)=C2C=C1)CCN3CCN(C(OCC4=CC(Cl)=CC(Cl)=C4)=O)CC3 |
| Molecular weight | 478,3 |
| Custom code | 2918.99 |
| Formulation | A crystalline solid |
| Purity | ≥95% |
| UNSPSC code | 12352100 |
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.
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(+)-D-threo-PDMP is a ceramide analog and is one of the four possible stereoisomers of PDMP (Item No. 62595).{11392} (+)-D-threo-PDMP is...
24(S),25-epoxy Cholesterol is an oxysterol and the most abundant oxysterol in mouse ventral midbrain.{43943} It activates liver X receptors (LXRs)...
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The Cayman COX Inhibitor Pack contains a combination of frequently used cyclooxygenase (COX) inhibitors. Each kit contains aspirin, the archetype...
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GST-tag Polyclonal Antibody (FITC) is a probe for the immunochemical detection of GST tags on recombinant proteins. Recombinant proteins are...
This rabbit anti-mouse IgA FITC is used as the ‘secondary antibody’ for immunostaining experiments where the primary antibody is mouse...
Cytosolic PGE synthase (cPGES) is a glutathione-dependent enzyme with a predicted size of 18.6 kDa (23 kDa on SDS-PAGE). The...
This mixture contains the primary COX products produced by most mammalian tissues. Contents: Prostaglandin D2, Prostaglandin E2, 6-keto Prostaglandin F1?,...
This mixture contains the characteristic metabolites of both PGI2 and TXA2. Contents: Thromboxane B2, 11-dehydro Thromboxane B2, 6-keto Prostaglandin F1?,...
Proprotein convertase subtilisin kexin 9 (PCSK9) is a member of the subtilisin serine protease family with an important role in...
Protein phosphorylation is an important post-translational modification that serves many key functions to regulate a protein’s activity, localization, and protein-protein...
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