NP3-562
Based on 1 Customer Validation
NP3-562 is an orally active NLRP3 Inhibitor. NP3-562 inhibits IL-1β release in the supernatant of Nigericin (HY-127019)-stimulated THP-1 cells (IC50 = 66 nM), human whole blood (IC50 = 214 nM) and a mouse acute peritonitis model. NP3-562 can be used for the study of acute peritonitis.
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- Purity: 98.16%
- CAS No.: 2409825-32-5
- 화학식: C19H24ClN5O3S
- 분자량:437.94
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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NLRP3 |
IL-1β 66 nM (IC50) |
| Species | Dose | Route | CL | Vss | T1/2 | AUC | F |
|---|---|---|---|---|---|---|---|
| Dog[1] | 0.1 mg/kg | i.v. | 12.4 mL/min/kg | 4.1 L/kg | 5.7 h | / | / |
| Dog[1] | 1 mg/kg | p.o. | / | / | / | 2530 μM·h | 89 % |
| Mice[1] | 1 mg/kg | i.v. | 85 mL/min/kg | 3.9 L/kg | 1 h | / | / |
| Mice[1] | 3 mg/kg | p.o. | / | / | / | 235 μM·h | 36 % |
| Rat[1] | 1 mg/kg | i.v. | 34 mL/min/kg | 5.5 L/kg | 3.5 h | / | / |
| Rat[1] | 10 mg/kg | p.o. | / | / | / | 712 μM·h | 63 % |
NP3-562 (50 mg/kg, p.o., single dose) exhibits brain exposure of 0.398 μM, thus demonstrating that it reaches also the central nervous system (CNS) with a brain-to-plasma ratio (Kp) of 0.2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute peritonitis model established in female C57BL/6 mice, 6-8 weeks of age[1]
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Dosage:3, 10, 30 and 100 mg/kg
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Administration:Oral administration (p.o.), single dose
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Result:Showed robust, dose-dependent inhibition of IL-1β in this model, with greater than 90% inhibition at 100 and 30 mg/kg, whereas dose-underproportional exposure and reduced efficacy were observed at 10 mg/kg dose.
Chemical Information
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CAS No. 2409825-32-5
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Appearance Solid
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분자량 437.94
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화학식 C19H24ClN5O3S
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Color White to light yellow
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SMILES
CC(O)(C(N1C2=C(SC(Cl)=C2)C=C13)=NN(CC(N[C@H]4CN(CCC4)C)=O)C3=O)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (228.34 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 (5.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (274 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 | 2.2834 mL | 11.4171 mL | 22.8342 mL | 57.0854 mL |
| 5 mM | 0.4567 mL | 2.2834 mL | 4.5668 mL | 11.4171 mL | |
| 10 mM | 0.2283 mL | 1.1417 mL | 2.2834 mL | 5.7085 mL | |
| 15 mM | 0.1522 mL | 0.7611 mL | 1.5223 mL | 3.8057 mL | |
| 20 mM | 0.1142 mL | 0.5709 mL | 1.1417 mL | 2.8543 mL | |
| 25 mM | 0.0913 mL | 0.4567 mL | 0.9134 mL | 2.2834 mL | |
| 30 mM | 0.0761 mL | 0.3806 mL | 0.7611 mL | 1.9028 mL | |
| 40 mM | 0.0571 mL | 0.2854 mL | 0.5709 mL | 1.4271 mL | |
| 50 mM | 0.0457 mL | 0.2283 mL | 0.4567 mL | 1.1417 mL | |
| 60 mM | 0.0381 mL | 0.1903 mL | 0.3806 mL | 0.9514 mL | |
| 80 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.7136 mL | |
| 100 mM | 0.0228 mL | 0.1142 mL | 0.2283 mL | 0.5709 mL |
NP3-562 Related Classifications
HY-163159 Related Classifications
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