sCSF1Rinh
Published date: 2022-06-22 21:57:40
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Name | GENZ-882706 | CAS# | 2070864-35-4 |
|---|---|---|---|---|
| Price | $Inquiry/100mg $Inquiry/250mg $Inquiry/1g | Purity | 98.0% | |
| Stocking Period |
3 Day | Stock | 3 | |
| Product Webpage: | https://www.dcchemicals.com/product_show-scsf1rinh.html | |||
| Detail
Product Information
sCSF1Rinh is a CNS-penetrant, potent and selective small-molecule CSF1R inhibitor, binds to CSF1R in a DFG-out conformation.is highly selective for CSF1R as compared to other kinases with a selectivity score of S(35)=0.005, sCSF1Rinh exhibited excellent pharmacokinetic properties including good oral bioavailability and CNS penetrance.sCSF1Rinh (500 nM) blocks these phosphorylation events in CSF1 (100 ng/mL) stimulation of BV2 microglia.sCSF1Rinh inhibited murine bone marrow-derived macrophage proliferation with IC50 of 22 nM, sCSF1Rinh significantly depletes microglia in a concentration-dependent manner in murine mixed glial cultures (IC50=188 nM).sCSF1Rinh reduced the number of microglia and infiltrating macrophages in an acute LPS model, with diminished microglial/macrophage proliferation and attenuated inflammatory response.sCSF1Rinh also suppressed a deleterious microglial response in the C57BL/6 EAE (experimental autoimmune encephalomy) model as well as the MOG peptide-induced non-obese diabetic EAE model of progressive MS (NOD-EAE) and improved neurological impairments in both models. |
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