Emlenoflast (MCC7840) sodium是磺酰脲类化合物,是一种NLRP3炎症小体 (NLRP3 inflammasome) 的选择性抑制剂,IC50值小于 100 nM, 可用于研究炎性疾病。
产品描述
Emlenoflast (MCC7840) sodium is a sulfonylurea that 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 [1] [2].
体外活性
Emlenoflast is an MCC950 analogue that shows useful activity in the inhibition of activation of the NLRP3 inflammasome, with an IC 50 of<100 nM [1].
体内活性
Emlenoflast (4 mg/kg; i.v.) shows the half-life (3.39 h), AUC 0-last (107097 ng h/mL) and CL (0.621 mL/min/kg) in mice [2]. Emlenoflast (20 mg/kg; p.o.) shows the oral bioavailability (67.2%), C max (60467 ng/mL) and half-life (5.02 h) in mice [2]. Animal Model: Male C57BL/6 mice (7-9 weeks) [2] 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.
Cas No.
2380032-29-9
分子式
C19H23N4NaO3S
分子量
410.47
别名
Emlenoflast sodium
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years