NIC-0102
Based on 1 Customer Validation
NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β.
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- Pureza: 98.79%
- No. CAS: 2806031-94-5
- Fòrmula: C21H25BF2N2O4
- Peso molecular:418.24
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Actividad biológica
|
proteasom β5 3.7 nM (IC50) |
proteasom β2 100.5 nM (IC50) |
proteasom β1 113.6 nM (IC50) |
NIC-0102 (compound 27) (7.5, 15, 30, 60 nM; 1h) specifically suppresses NLRP3 inflammasome activation in LPS-primed J774A.1 and BMDM cells[1].
NIC-0102 (7.5, 15, 30, 60 nM; 1h) induces polyubiquitination of NLRP3 via inhibition of the proteasome during the activation step in LPS-primed J774A.1 cells[1].
NIC-0102 (7.5, 15, 30, 60 nM; 1h) exhibits inhibitory effects on NF-κB in the priming step of the NLRP3 pathway in LPS-primed J774A.1 cells[1].
NIC-0102 (15, 60 nM; 1h) blocks NLRP3-ASC interaction and ASC oligomerization in LPS-primed J774A.1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:J774A.1 and BMDM cells (LPS-primed)
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Concentration:7.5, 15, 30, 60 nM
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Incubation Time:1 h
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Result:Inhibited the release of IL-1β in a dose-dependent manner.
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Cell Line:J774A.1 cells (LPS-primed)
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Concentration:7.5, 15, 30, 60 nM
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Incubation Time:1 h
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Result:Dose-dependently inhibited the release of mature IL-1β and the caspase-1 p20 subunit in supernatants from J774A.1 cells but did not affect pro-IL-1β, pro-caspase-1, NLRP3, or ASC in cell lysates.
Increased the polyubiquitinated NLRP3 protein in adose-dependent manner, and significantly increased the amount of c-Cbl and Cbl-b.
Showed an inhibitory effect on the NF-κB subunit p65, phosphorylated p65, and NLRP3 protein at 60 nM, at which NF-κB-dependent TNF-α secretion was slightly decreased.
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Cell Line:J774A.1 cells (LPS-primed)
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Concentration:15, 60 nM
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Incubation Time:1 h
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Result:Inhibited the interaction between NLRP3and ASC stimulated by LPS and nigericin.
Showed a concentration-dependent suppression effect on ASC oligomerization.
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 (6 to 8-week-old; DSS-induced ulcerative colitis model)[1].
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Dosage:0.125, 0.25, and 0.5 mg/kg
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Administration:Oral gavage; single every 72 h for 10 days.
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Result:Significantly suppressed weight and fecal occult blood.
Decreased colonic length in a dose-dependent manner.
Resulted in a dose-dependent reduction in tissue-associated IL-1β concentration and significantly inhibited pro-IL-1β.
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Animal Model:Male C57BL/6 mice (6 to 8-week-old)[1].
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Dosage:0.5 mg/kg (for i.v.); 1 mg/kg (for p.o.)
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Administration:Intravenous injection; Oral gavage; single.
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Result:
1.19 Pharmacokinetic Parameters of NIC-0102 in male C57BL/6 mice[1].
IV (0.5 mg/kg) PO (1 mg/kg) T1/2 (h) 4.73 8.36 Tmax (h) 0.08 0.25 Cmax (ng/mL) 376.6 207.7 AUC0-∞ (h•ng/mL) 448.8 489.2 MRT0-∞ (h) 6.14 - Vz (L/kg) 7.7 - CL (mL/min/kg) 18.8 - F (%) - 48.1%
Chemical Information
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No. CAS 2806031-94-5
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Appearance Solid
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Peso molecular 418.24
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Fòrmula C21H25BF2N2O4
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Color White to off-white
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SMILES
CC(C[C@@H](B(O)O)NC([C@@H](NC(C1=C(C=CC=C1F)F)=O)CC2=CC=CC=C2)=O)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (239.10 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. 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.98 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.3910 mL | 11.9549 mL | 23.9097 mL | 59.7743 mL |
| 5 mM | 0.4782 mL | 2.3910 mL | 4.7819 mL | 11.9549 mL | |
| 10 mM | 0.2391 mL | 1.1955 mL | 2.3910 mL | 5.9774 mL | |
| 15 mM | 0.1594 mL | 0.7970 mL | 1.5940 mL | 3.9850 mL | |
| 20 mM | 0.1195 mL | 0.5977 mL | 1.1955 mL | 2.9887 mL | |
| 25 mM | 0.0956 mL | 0.4782 mL | 0.9564 mL | 2.3910 mL | |
| 30 mM | 0.0797 mL | 0.3985 mL | 0.7970 mL | 1.9925 mL | |
| 40 mM | 0.0598 mL | 0.2989 mL | 0.5977 mL | 1.4944 mL | |
| 50 mM | 0.0478 mL | 0.2391 mL | 0.4782 mL | 1.1955 mL | |
| 60 mM | 0.0398 mL | 0.1992 mL | 0.3985 mL | 0.9962 mL | |
| 80 mM | 0.0299 mL | 0.1494 mL | 0.2989 mL | 0.7472 mL | |
| 100 mM | 0.0239 mL | 0.1195 mL | 0.2391 mL | 0.5977 mL |
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