RIP2kinaseinhibitor2是一种受体相互作用蛋白-2(RIP2)激酶抑制剂,详细信息请参考专利WO/2014043437A1中的化合物example9。
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RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9.
RIP2 kinase inhibitor 2 is a novel prodrug of a quinazolyl amine that inhibits RIP2 kinase. Receptor interacting protein-2 (RIP2) kinase is a TKL family serine/threonine protein kinase involved in innate immune signaling. Following activation, RIP2 kinase associates with NODI or NOD2 and appears to function principally as a molecular scaffold to bring together other kinases (TAK1, Ικκα/β/γ) involved in NF-κβ and mitogen-activated protein kinase activation[1].
[1]. Linda N. Casillas, et al. Amino-quinolines as kinase inhibitors. PCT Int. Appl. (2014), WO 2014043437 A1 20140320.
Animal experiment: | Rats[1] Rats are orally pre-dosed with the RIP2 kinase inhibitor 2, at doses of 0.016, 0.16 and 1.6 mg/kg (n=8 rats/group), followed by dosing with L18-MDP (50 μg/rat) 0.25 hours after pre-dosing with the compound. The IL8 cytokine levels and percentage levels are calculated as the mean±standard error of the mean (n=8 rats/group). |
参考文献: [1]. Linda N. Casillas, et al. Amino-quinolines as kinase inhibitors. PCT Int. Appl. (2014), WO 2014043437 A1 20140320. |
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