NLRP3-IN-79
Based on 1 Customer Validation
NLRP3-IN-79 is an orally active NLRP3 inhibitor. NLRP3-IN-79 inhibits NLRP3 inflammasome with an IC50 of 10.69 nM. NLRP3-IN-79 blocks NLRP3 inflammasome assembly by directly binding to NLRP3 and disrupting the NEK7-NLRP3 interaction. NLRP3-IN-79 can be used for the study of NLRP3-driven diseases model, including systemic inflammation, peritonitis, and colitis.
For research use only. We do not sell to patients.
- Purity: 99.10%
- CAS No.: 3088796-72-6
- Formula: C23H28N4O2
- Molecular Weight:392.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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NLRP3 inflammasome 10.69 nM (IC50) |
NEK7 |
IL-18 |
IL-1β |
NLRP3-IN-79 (compound B6) (3-30 nM, 5 h 45 min) inhibits activation and assembly of NLRP3 inflammasome in Lipopolysaccharide (LPS) (HY-D1056) (100 ng/mL, 4 h) + Adenosine triphosphate (ATP) (HY-B2176) (5 mM, 45 min) induced human and bone macrophages[1].
NLRP3-IN-79 (3-30 nM, 1 h) blocks NLRP3 inflammasome assembly by disrupting NEK7-NLRP3 interaction in LPS (100 ng/mL, 4 h) + ATP (5 mM, 45 min) induced BMDMs[1].
NLRP3-IN-79 (0-500 μM, 20 h) has no significant hepatocellular toxicity in AML-12 and HL-7702[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS + ATP induced HMDMs and BMDMs
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Concentration:3, 10, and 30 nM was applied to LPS-primed (100 ng/mL, 4 h) prior to ATP stimulation (5 mM, 45 min)
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Incubation Time:5 h 45 min
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Result:Markedly reduced the caspase-1 cleavage and IL-1β maturation.
Reduced secretion of IL-1β and IL-18.
Markedly reduced the caspase-1 cleavage and IL-1β maturation triggered by both nigericin and monosodium urate.
Reduced secretion of IL-1β and IL-18.
Inhibited formation of NLRP3/ASC/Pro-caspase-1 complexes.
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Cell Line:LPS + ATP induced BMDMs
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Concentration:3, 10, and 30 nM was applied to LPS-primed (100 ng/mL, 4 h) prior to ATP stimulation (5 mM, 45 min)
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Incubation Time:5 h 45 min
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Result:Attenuated ATP-induced ASC oligomerization.
Disrupted the interaction of NEK7-NLRP3 in a concentration-dependent manner.
NLRP3-IN-79 (5-20 mg/kg, i.p., once) mitigates Monosodium urate (MSU) (HY-B2130A)-induced peritonitis in C57BL/6 mice[1].
NLRP3-IN-79 (5-20 mg/kg, o.p., 10 days) markedly alleviates Dextran sulfate sodium salt (DSS) (HY-116282C)-induced colitis in female C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS (20 mg/kg, i.p., once) induced inflammatory model in female C57BL/6 mice (6-8 weeks, 18-20 g)[1].
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Dosage:5, 10, 20 mg/kg
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Administration:i.p., 1 h before LPS administration, blood samples were collected for detecting 2 h after LPS administration.
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Result:Reduced IL-1β production in both serum and peritoneal lavage fluid.
Reduced proportion of neutrophils in the peritoneal lavage fluids.
Ameliorated LPS-induced systemic inflammation in mice.
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Animal Model:MSU (30 mg/kg, i.p., once) induced inflammatory mode in female C57BL/6 mice (6-8 weeks, 18-20 g)[1].
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Dosage:5; 10; 20 mg/kg
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Administration:i.p., before MSU induction.
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Result:Inhibited infiltration of neutrophils in the peritoneal lavage fluid.
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Animal Model:DSS (2.8%, p.o., 10 days) induced inflammatory model in female C57BL/6 mice (6-8 weeks old, 18-20 g)[1].
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Dosage:5, 10, 20 mg/kg
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Administration:i.p., for 10 consecutive days.
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Result:Inhibited infiltration of neutrophils in the peritoneal lavage fluid.
Chemical Information
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CAS No. 3088796-72-6
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Appearance Solid
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Molecular Weight 392.49
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Formula C23H28N4O2
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Color Light yellow to yellow
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SMILES
CCNC(N(CC1=CN=CC=C1)CC(NC2=C3C(CCC3)=CC4=C2CCC4)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (254.78 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 2.5478 mL | 12.7392 mL | 25.4784 mL | 63.6959 mL |
| 5 mM | 0.5096 mL | 2.5478 mL | 5.0957 mL | 12.7392 mL | |
| 10 mM | 0.2548 mL | 1.2739 mL | 2.5478 mL | 6.3696 mL | |
| 15 mM | 0.1699 mL | 0.8493 mL | 1.6986 mL | 4.2464 mL | |
| 20 mM | 0.1274 mL | 0.6370 mL | 1.2739 mL | 3.1848 mL | |
| 25 mM | 0.1019 mL | 0.5096 mL | 1.0191 mL | 2.5478 mL | |
| 30 mM | 0.0849 mL | 0.4246 mL | 0.8493 mL | 2.1232 mL | |
| 40 mM | 0.0637 mL | 0.3185 mL | 0.6370 mL | 1.5924 mL | |
| 50 mM | 0.0510 mL | 0.2548 mL | 0.5096 mL | 1.2739 mL | |
| 60 mM | 0.0425 mL | 0.2123 mL | 0.4246 mL | 1.0616 mL | |
| 80 mM | 0.0318 mL | 0.1592 mL | 0.3185 mL | 0.7962 mL | |
| 100 mM | 0.0255 mL | 0.1274 mL | 0.2548 mL | 0.6370 mL |
NLRP3-IN-79 Related Classifications
HY-174270 Related Classifications
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