ChemicalBook > CAS DataBase List > 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
- Product Name
- N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl) amino]carbonyl]-1-(1-methylethyl)-1H-Pyrazole-3-sulfonamide
- CAS No.
- 1995067-59-8
- Chemical Name
- N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl) amino]carbonyl]-1-(1-methylethyl)-1H-Pyrazole-3-sulfonamide
- Synonyms
- MCC7840;Emlenoflast;MCC7840 sodium;Inzomelid;N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-1-isopropyl-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;1H-Pyrazole-3-sulfonamide, N-[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl)amino]carbonyl]-1-(1-methylethyl)-;MCC 7840,sulfonylurea,Emlenoflast,NLRP3,inhibit,NOD-like Receptor (NLR),MCC-7840,inflammatory,inflammasome,Inhibitor
- CBNumber
- CB88058517
- Molecular Formula
- C19H24N4O3S
- Formula Weight
- 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 Property
- 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 Chemical Properties,Usage,Production
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-sulfonamide Preparation Products And Raw materials
Raw materials
Preparation Products
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