Uses
Emlenoflast (MCC7840) sodium, a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. Emlenoflast sodium can be used for the research of inflammatory diseases[1][2].
Biological Activity
MCC7840 sodium, a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. MCC7840 sodium can be used for the research of inflammatory diseases[1][2].
MCC7840, a MCC950 analogue, shows useful activity in the inhibition of activation of the NLRP3 inflammasome, with an IC50 of <100 nM[1].
MCC7840 (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[2].MCC7840 (20 mg/kg; p.o.) exhibits the oral bioavailability (67.2%), Cmax (60467 ng/mL) and half-life (5.02 h) in mice[2].
in vivo
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[2].
?
Emlenoflast (20 mg/kg; p.o.) exhibits the oral bioavailability (67.2%), Cmax (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.: 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.
|
IC 50
NLRP3 inflammasome: <100 nM (IC50)
storage
-20°C, away from moisture
References
[1]. El-Sharkawy LY, et, al. Inhibiting the NLRP3 Inflammasome. Molecules. 2020 Nov 25;25(23):5533. [2]. O’neill L, et, al. Sulfonylureas and related compounds and use of same. WO2016131098A1.
