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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
Emlenoflast (MCC7840) sodium, a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome , with an IC 50 of <100 nM. Emlenoflast sodium can be used for the research of inflammatory diseases
In Vitro
Emlenoflast, a MCC950 analogue, shows useful activity in the inhibition of activation of the NLRP3 inflammasome, with an IC 50 of <100 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Emlenoflast (4 mg/kg; i.v.) exhibits the half-life (3.39 h), AUC 0-last (107097 ng?h/mL) and CL (0.621 mL/min/kg) in mice. ?\nEmlenoflast (20 mg/kg; p.o.) exhibits the oral bioavailability (67.2%), C max (60467 ng/mL) and half-life (5.02 h) in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6 mice (7-9 weeks)Dosage: 4 mg/kg for i.v. and 20 mg/kg for p.o. (Pharmacokinetic Analysis) Administration: A single intravenousbolus or oral gavage Result: I.v.: t 1/2 =3.39 h; AUC 0-last =107097 ng•h/mL; CL=0.621 mL/min/kg. P.o.: F=67.2%; C max =60467 ng/mL; t 1/2 =5.02 h.
Form:Solid
IC50& Target:NLRP3 inflammasome <100 nM (IC 50 )