| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
(rac)-NDT-19795 targets the NLRP3 (NOD-like receptor family pyrin domain containing 3) inflammasome, a multiprotein complex that plays a key role in innate immunity and inflammation. The NLRP3 inflammasome is activated by various danger signals and triggers the maturation and secretion of pro-inflammatory cytokines IL-1beta and IL-18, leading to pyroptotic cell death. NDT-19795 is an effective inhibitor of NLRP3, blocking its activation and downstream signaling. It is a carboxylic acid active substance that can be converted from NT-0796 within cells.
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| ln Vitro |
NDT-19795 is an effective inhibitor of the NLRP3 inflammasome with an IC50 of 66 nM in the PBMC method (peripheral blood mononuclear cells) and an IC50 of 4.7 microM in the Western blot (WB) method. (rac)-NDT-19795 is the racemate of NDT-19795. The compound is a carboxylic acid active substance, which can be intracellularly converted from NT-0796. NDT-19795 can be used for studies of inflammation and neurological diseases. Western blot (WB) method measures the inhibition of IL-1beta secretion in LPS/ATP-stimulated THP-1 cells.
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| ln Vivo |
In vivo, NDT-19795, the active moiety of the prodrug NT-0796, would be expected to inhibit NLRP3 inflammasome activation. It can be used for research on inflammatory and neurological disorders. As a carboxylic acid active substance, it is likely the active metabolite of the prodrug NT-0796. In animal models of inflammatory diseases (e.g., multiple sclerosis, colitis, gout), inhibition of NLRP3 would be expected to reduce IL-1beta levels and ameliorate disease severity. The compound is applicable in studies of inflammation and neurological diseases.
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| Enzyme Assay |
In vitro NLRP3 inflammasome inhibition assay (ELISA): Human THP-1 monocytes are differentiated into macrophages using PMA (50 ng/mL) for 48-72 hours. Cells are seeded in 96-well plates (1×10⁵ cells/well). The cells are first primed with LPS (100 ng/mL) for 4 hours to induce pro-IL-1beta expression. Varying concentrations of (rac)-NDT-19795 (0.01-1000 uM) are then added for 30 min, followed by ATP (5 mM) stimulation for 30 min to activate the NLRP3 inflammasome. The supernatant is collected, and IL-1beta secretion is quantified by ELISA. The IC₅0 (66 nM) is calculated from the dose-response curve. Cytotoxicity is assessed by LDH release.
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| Cell Assay |
In vitro Western blot for IL-1beta processing: THP-1 macrophages are primed with LPS (100 ng/mL) for 4 hours, then treated with varying concentrations of (rac)-NDT-19795 (0.1-100 uM) for 30 min, followed by ATP (5 mM) for 30 min. Cell lysates are collected, and cleaved IL-1beta (p17) and pro-IL-1beta are detected by Western blotting. The IC₅0 for inhibition of IL-1beta maturation (4.7 uM) is calculated by densitometry. This method is used as an orthogonal confirmation of NLRP3 inhibition, as the PBMC method (ELISA) is more sensitive.
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| Animal Protocol |
In vivo model of NLRP3-driven inflammation (e.g., MSU crystal-induced peritonitis): Male C57BL/6 mice (6-8 weeks old, n=8-10/group) are used. The active compound NDT-19795 (or the prodrug NT-0796) is administered orally or intraperitoneally at doses of 10-100 mg/kg 1 hour before challenge. Peritonitis is induced by intraperitoneal injection of monosodium urate (MSU) crystals (1 mg/mouse) or alum. After 4-6 hours, mice are euthanized, and the peritoneal cavity is lavaged with PBS. IL-1beta levels in the lavage fluid are measured by ELISA. The number of neutrophils recruited is assessed by flow cytometry or by counting cells in a hemocytometer. This model is used to evaluate in vivo NLRP3 inhibition.
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| ADME/Pharmacokinetics |
No specific PK data for (rac)-NDT-19795 is available. The compound is the active carboxylic acid metabolite of the prodrug NT-0796. NT-0796 is cell-permeable and is converted intracellularly to NDT-19795 by esterase-mediated hydrolysis. The half-life of NDT-19795 in plasma and tissues would depend on the rate of conversion and clearance. The compound is expected to have a short half-life (< 2 h) due to rapid clearance. NDT-19795 is a carboxylic acid, which may undergo glucuronidation (Phase II metabolism) and be excreted in urine. For research use, the compound is typically formulated in DMSO for in vitro studies.
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| Toxicity/Toxicokinetics |
For (rac)-NDT-19795, hazard statements: H315 (Causes skin irritation), H319 (Causes serious eye irritation), H335 (May cause respiratory irritation). Signal word: Warning. Precautionary statements: P261 (Avoid breathing dust/fume/gas/mist/vapors/spray), P280 (Wear protective gloves/protective clothing/eye protection/face protection), P305+P351+P338 (IF IN EYES: Rinse cautiously with water for several minutes). Storage: powder at -20degC, protected from light and moisture. For research use only, not for human consumption.
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| References | |
| Additional Infomation |
(rac)-NDT-19795 (CAS# 2272918-42-8) is a research-grade racemate of the potent NLRP3 inflammasome inhibitor NDT-19795 (IC50 = 66 nM in PBMCs). It is used for research on inflammatory and neurological disorders, including multiple sclerosis, Alzheimer's disease, and gout. It is not an FDA-approved drug. For research use only, not for diagnostic or therapeutic applications.
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| Molecular Formula |
C20H21N3O4
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| Molecular Weight |
367.40
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| CAS # |
2272918-42-8
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| Related CAS # |
NDT-19795; (S)-NDT-19795
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| Appearance |
White to off-white solid powder
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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) |
DMSO : ~100 mg/mL (~272.18 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.80 mM)(saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one)),clear solution.
For example, if 1 mL of working solution is to be prepared, you can Add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix thoroughly. Then add 50 μL of Tween-80 to the above system and mix thoroughly. Finally, add 450 μL of physiological saline to bring the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in ddH₂O and bring the volume to 100 mL to obtain a clear and transparent physiological saline solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.80 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one)),clear solution. For example, if 1 mL of working solution is to be prepared, you can Add 100 μL of 25.0 mg/mL clarified DMSO stock solution to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7218 mL | 13.6091 mL | 27.2183 mL | |
| 5 mM | 0.5444 mL | 2.7218 mL | 5.4437 mL | |
| 10 mM | 0.2722 mL | 1.3609 mL | 2.7218 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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