Emlenoflast
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 99.30%
- CAS No.: 1995067-59-8
- Formula: C19H24N4O3S
- Molecular Weight:388.48
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
Description
IC50 & Target
[1]|
NLRP3 inflammasome <100 nM (IC50) |
In Vitro
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (7-9 weeks)[2]
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Dosage:4 mg/kg for i.v. and 20 mg/kg for p.o. (Pharmacokinetic Analysis)
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Administration:A single intravenousbolus or oral gavage
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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.
Chemical Information
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CAS No. 1995067-59-8
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Appearance Solid
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Molecular Weight 388.48
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Formula C19H24N4O3S
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Color White to off-white
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SMILES
O=S(C1=NN(C(C)C)C=C1)(NC(NC2=C3CCCC3=CC4=C2CCC4)=O)=O
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Synonyms
MCC7840
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (257.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5741 mL | 12.8707 mL | 25.7414 mL | 64.3534 mL |
| 5 mM | 0.5148 mL | 2.5741 mL | 5.1483 mL | 12.8707 mL | |
| 10 mM | 0.2574 mL | 1.2871 mL | 2.5741 mL | 6.4353 mL | |
| 15 mM | 0.1716 mL | 0.8580 mL | 1.7161 mL | 4.2902 mL | |
| 20 mM | 0.1287 mL | 0.6435 mL | 1.2871 mL | 3.2177 mL | |
| 25 mM | 0.1030 mL | 0.5148 mL | 1.0297 mL | 2.5741 mL | |
| 30 mM | 0.0858 mL | 0.4290 mL | 0.8580 mL | 2.1451 mL | |
| 40 mM | 0.0644 mL | 0.3218 mL | 0.6435 mL | 1.6088 mL | |
| 50 mM | 0.0515 mL | 0.2574 mL | 0.5148 mL | 1.2871 mL | |
| 60 mM | 0.0429 mL | 0.2145 mL | 0.4290 mL | 1.0726 mL | |
| 80 mM | 0.0322 mL | 0.1609 mL | 0.3218 mL | 0.8044 mL | |
| 100 mM | 0.0257 mL | 0.1287 mL | 0.2574 mL | 0.6435 mL |