RA03546849 (CSF1Rinh, GENZ-882706) | CSF1R inhibitor | Probechem Biochemicals

Chemical Structure : RA03546849

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RA03546849 (GENZ-882706, sCSF1Rinh)

货号: PC-72412Not For Human Use, Lab Use Only.

RA03546849 (CSF1Rinh, GENZ-882706) is a CNS-penetrant, potent and selective small-molecule CSF1R inhibitor, binds to CSF1R in a DFG-out conformation.

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生物&药学活性

RA03546849 (CSF1Rinh, GENZ-882706) is a CNS-penetrant, potent and selective small-molecule CSF1R inhibitor, binds to CSF1R in a DFG-out conformation.
RA03546849 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.

物理化学性质&存储条件

分子量	455.518
分子式	C26H25N5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-4-(3-((2-(6-methoxypyridin-3-yl)-2,3-dihydrobenzo[b][1,4] dioxin-6-yl)methyl)-3H-imidazo [4,5-b]pyridin-6-yl)-2-methylbut-3-yn-2-amine

参考文献

1. Nellwyn Hagan, et al. Cell Death Dis. 2020 Oct 23;11(10):904.

RA03546849 (GENZ-882706, sCSF1Rinh)

生物&药学活性

物理化学性质&存储条件

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RA03546849 (GENZ-882706, sCSF1Rinh)

生物&药学活性

物理化学性质&存储条件

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