| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
NLRP3
NLRP3 (NOD-, LRR- and pyrin domain-containing protein 3), a key component of the NLRP3 inflammasome. NP3-146 (NLRP3-IN-5) is an inflammasome NLRP3 inhibitor. By inhibiting NLRP3, the compound blocks the assembly and activation of the NLRP3 inflammasome, reducing the production of pro-inflammatory cytokines such as IL-1β and IL-18. This makes NP3-146 a potential therapeutic agent for autoimmune and inflammatory diseases. |
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| ln Vitro |
In vitro, NP3-146 is an NLRP3 inflammasome inhibitor. The compound inhibits NLRP3-mediated inflammatory responses, including the production of IL-1β and other pro-inflammatory cytokines. By blocking NLRP3 inflammasome activation, NP3-146 reduces the inflammatory cascade that contributes to autoimmune and inflammatory diseases.
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| ln Vivo |
In vivo, NP3-146 can be used for the study of autoimmune diseases. By inhibiting NLRP3 inflammasome activation, the compound may reduce inflammation and tissue damage in autoimmune conditions. However, detailed in vivo efficacy data in specific animal models of autoimmune diseases are limited in the available literature.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for NP3-146 is not a typical enzyme inhibition assay, as NLRP3 is not an enzyme but a scaffolding protein. Instead, the compound's activity is assessed in cell-based assays measuring NLRP3 inflammasome activation. The binding of NP3-146 to NLRP3 could potentially be assessed using biophysical techniques, but such assays are not described in the available literature.
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| Cell Assay |
In vitro cellular assays for NP3-146 are performed using macrophages or other cell types that express NLRP3. Cells are primed with LPS and then stimulated with an NLRP3 activator in the presence of varying concentrations of the compound. IL-1β production is measured in the culture supernatant by ELISA. The compound's ability to inhibit NLRP3-mediated IL-1β secretion is assessed, and the IC50 is determined from dose-response curves.
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| Animal Protocol |
In vivo animal experiments for NP3-146 would typically be conducted in rodent models of autoimmune diseases, such as experimental autoimmune encephalomyelitis (EAE), collagen-induced arthritis (CIA), or lupus-prone mice. The compound would be administered via oral gavage or intraperitoneal injection. Pharmacodynamic endpoints would include the measurement of IL-1β and other inflammatory cytokines in serum or tissues, assessment of NLRP3 inflammasome activation markers, and evaluation of disease severity using clinical scores or histopathological assessment.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for NP3-146 are limited. As a small molecule, the compound is expected to have moderate oral bioavailability and tissue distribution. However, detailed pharmacokinetic parameters such as half-life, Cmax, AUC, and clearance have not been extensively reported. Further studies would be required to fully characterize its ADME properties.
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| Toxicity/Toxicokinetics |
Toxicology data for NP3-146 are limited. The compound is used for research purposes only and is not approved for human use. No significant toxicities have been reported in the available literature. As an NLRP3 inhibitor, the compound may have immunomodulatory effects that could impact host defense against infections. Careful evaluation of safety and potential off-target effects would be required for therapeutic development.
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| References | |
| Additional Infomation |
NP3-146 (CAS: 210826-47-4) is an inflammasome NLRP3 inhibitor with potential anti-inflammatory activity. It is also known as NLRP3-IN-5. NP3-146 can be used for the study of autoimmune diseases. The compound is not approved for human use and is intended for research purposes only.
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| Molecular Formula |
C20H27CLN2O5S
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|---|---|
| Molecular Weight |
442.96
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| Exact Mass |
442.132
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| CAS # |
210826-47-4
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| PubChem CID |
10195003
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
659
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)C1=CC(=CC(=C1NC(=O)NS(=O)(=O)C2=CC(=CO2)C(C)(C)O)C(C)C)Cl
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| InChi Key |
RTJGVFANTDWUEG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H27ClN2O5S/c1-11(2)15-8-14(21)9-16(12(3)4)18(15)22-19(24)23-29(26,27)17-7-13(10-28-17)20(5,6)25/h7-12,25H,1-6H3,(H2,22,23,24)
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| Chemical Name |
1-[4-chloro-2,6-di(propan-2-yl)phenyl]-3-[4-(2-hydroxypropan-2-yl)furan-2-yl]sulfonylurea
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2575 mL | 11.2877 mL | 22.5754 mL | |
| 5 mM | 0.4515 mL | 2.2575 mL | 4.5151 mL | |
| 10 mM | 0.2258 mL | 1.1288 mL | 2.2575 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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