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ChemicalBook >  Product Catalog >  Organic Chemistry >  Heterocyclic Compounds >  N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl) amino]carbonyl]-1-(1-methylethyl)-1H-Pyrazole-3-sulfonamide

N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl) amino]carbonyl]-1-(1-methylethyl)-1H-Pyrazole-3-sulfonamide

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N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl) amino]carbonyl]-1-(1-methylethyl)-1H-Pyrazole-3-sulfonamide Basic information

Product Name:
N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl) amino]carbonyl]-1-(1-methylethyl)-1H-Pyrazole-3-sulfonamide
Synonyms:
  • N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl) amino]carbonyl]-1-(1-methylethyl)-1H-Pyrazole-3-sulfonamide
  • 1H-Pyrazole-3-sulfonamide, N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl)amino]carbonyl]-1-(1-methylethyl)-
  • MCC7840 sodium
  • Emlenoflast
  • MCC7840
  • N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-1-isopropyl-1H-pyrazole-3-sulfonamide
  • MCC 7840,sulfonylurea,Emlenoflast,NLRP3,inhibit,NOD-like Receptor (NLR),MCC-7840,inflammatory,inflammasome,Inhibitor
  • Inzomelid
CAS:
1995067-59-8
MF:
C19H24N4O3S
MW:
388.48
Mol File:
1995067-59-8.mol
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N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl) amino]carbonyl]-1-(1-methylethyl)-1H-Pyrazole-3-sulfonamide Chemical Properties

Density 
1.46±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
pka
1.50±0.10(Predicted)
form 
Solid
color 
White to off-white
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N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl) amino]carbonyl]-1-(1-methylethyl)-1H-Pyrazole-3-sulfonamide Usage And Synthesis

Uses

Emlenoflast (MCC7840), a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. Emlenoflast can be used for the research of inflammatory diseases[1][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)

References

[1] El-Sharkawy LY, et, al. Inhibiting the NLRP3 Inflammasome. Molecules. 2020 Nov 25;25(23):5533. DOI:10.3390/molecules25235533
[2] O'neill L, et, al. Sulfonylureas and related compounds and use of same. WO2016131098A1.

N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl) amino]carbonyl]-1-(1-methylethyl)-1H-Pyrazole-3-sulfonamideSupplier

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