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PLX5622 is a brain-penetrant inhibitor of the colony stimulating factor 1 receptor (CSF1R; IC50 = 0.016 µM).{53727} It is selective for CSF1R over FMS-related tyrosine kinase 3 (FLT3), Kit, Aurora C, and VEGFR2 (IC50s = 0.39, 0.86, 1, and 1.1 µM, respectively) and is greater than 100-fold selective for CSF1R over a panel of 230 kinases.{53727,53728} PLX5622 (65 mg/kg) reduces the number of Iba-1+ cells, a marker of reduced microglia activation, in the dorsal horn of the spinal cord in a mouse model of neuropathic pain induced by partial ligation of the sciatic nerve.{53728} It also decreases macrophage levels of TNF-? and IL-1? and infiltration into the sciatic nerve, as well as alleviates mechanical and cold allodynia in the same model. Dietary administration of PLX5622 (1,200 ppm in chow) decreases the number of hippocampal microglia by 90%, as well as reduces the number and volume of retrosplenial and somatosensory cortical amyloid-? (A?) plaques in the 5XFAD transgenic mouse model of Alzheimer’s disease.{53727}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 25 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| Molecular formula | C21H19F2N5O • 1/2C4H4O4 |
| Smiles | CC1=CN=C(NC=C2CC3=CC=C(NCC4=C(OC)N=CC(F)=C4)N=C3F)C2=C1.OC(/C=C/C(O)=O)=O.CC5=CN=C(NC=C6CC7=CC=C(NCC8=C(OC)N=CC(F)=C8)N=C7F)C6=C5 |
| Molecular weight | 485,4 |
| Custom code | 2933.39 |
| Formulation | A solid |
| Purity | ≥98% |
| 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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Amyloid-? (1-8, A2V) is a truncated form of amyloid-? (A?) that contains a valine to alanine substitution at position 2...
Proprotein convertase subtilisin kexin 9 (PCSK9) is a member of the subtilisin serine protease family with an important role in...
Prostaglandin I synthase (PGIS) catalyzes the isomerization of PGH2 to PGI2. PGI2 (prostacyclin) is a potent vasodilator and inhibitor of...
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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...
The Cayman COX Inhibitor Pack contains a combination of frequently used cyclooxygenase (COX) inhibitors. Each kit contains aspirin, the archetype...
Histone H2A is a core histone that forms a dimer with histone H2B.{46631} Two histone H2A/H2B dimers form an octameric...
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