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Description: Potent brain penetrant inhibitor of the NLRP3 inflammasome
Chemical Name: 2-[6-[[(3R)-1-Ethyl-3-piperidinyl]amino]-3-pyridazinyl]-3-methyl-5-(trifluoromethyl)phenol
Purity: ≥98% (HPLC)
Biological Activity for NP3-253
NP3-253 is a potent NLRP3 inflammasome inhibitor (IL-1β IC50 = 0.7 nM and 8 nM in THP1-1 cells and whole blood, respectively). NP3-253 is brain-penetrant and displays promising physicochemical and PK properties, which differentiate it from previously described molecules.
NP3-253 blocks IL-1β production and IL-18 maturation and pyroptosis in vitro.
In vivo, NP3-253 shows inhibition of the NLRP3 inflammasome in the periphery and CNS and provides insights on free drug concentrations required to inhibit IL-1β production in the cerebrospinal fluid (CSF).
Technical Data for NP3-253
| M. Wt | 380.42 |
| Formula | C19H23F3N4O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2557349-50-3 |
| PubChem ID | 155284649 |
| InChI Key | UVVZGYXCKGWWCC-CQSZACIVSA-N |
| Smiles | CC1=C(C2=CC=C(N=N2)N[C@H]3CN(CCC3)CC)C(O)=CC(C(F)(F)F)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for NP3-253
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.04 | 100 |
Preparing Stock Solutions for NP3-253
The following data is based on the product molecular weight 380.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.63 mL | 13.14 mL | 26.29 mL |
| 5 mM | 0.53 mL | 2.63 mL | 5.26 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.63 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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Product Datasheets for NP3-253
Certificate of Analysis is currently unavailable on-line.
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References for NP3-253
References are publications that support the biological activity of the product.
MacKay et al (2024) Discovery of NP3-253, a potent brain penetrant inhibitor of the NLRP3 inflammasome. 67 20780 PMID: 39574318
If you know of a relevant reference for NP3-253, please let us know.
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