Emlenoflast

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Emlenoflast 是一种有效的、选择性的 NLRP3 炎症小体抑制剂。

Emlenoflast is a potent and selective inhibitor of NLRP3 inflammasome.

Emlenoflast, a MCC950 analogue, shows useful activity in the inhibition of activation of the NLRP3 inflammasome, with an IC50 of <100 nM.

Emlenoflast (4 mg/kg; i.v.) exhibits the half-life (3.39 h), AUC0-last (107097 ng?h/mL) and CL (0.621 mL/min/kg) in mice.Emlenoflast (20 mg/kg; p.o.) exhibits the oral bioavailability (67.2%), Cmax (60467 ng/mL) and half-life (5.02 h) in mice. 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.: t1/2=3.39 h; AUC0-last=107097 ng?h/mL; CL=0.621 mL/min/kg.P.o.: F=67.2%; Cmax=60467 ng/mL; t1/2=5.02 h.

MCC7840

NF-κB

NOD

NLRP3

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1995067-59-8

388.48

C19H24N4O3S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (321.77 mM)

O=S(C1=NN(C(C)C)C=C1)(NC(NC2=C3CCCC3=CC4=C2CCC4)=O)=O

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(-20℃)

With Ice Pack

≥ 2 years