NT-0527
Based on 1 Customer Validation
NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.80%
- No. CAS: 2771019-10-2
- Fòrmula: C17H14ClFN4O2
- Peso molecular:360.77
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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IL-1β 0.79 μM (IC50) |
CYP2C19 |
NLRP3 inflammasome |
NT-0527 (0.001-10 μM; 90 min) disrupts the formation of NLRP3 inflammasome and reduces IL-1β release in a dose-dependent manner in human PBMCs, with IC50 values of 0.062 μM, 0.087 μM and 0.040 μM for ATP, MSU (HY-B2130A) and CPPD stimulation, respectively[1].
NT-0527 (0.01-100 μM; 3.5 h) inhibits IL-1β production in a dose-dependent manner with a mean IC50 of 0.79 μM in human whole blood [1].
NT-0527 (250 nM, 1 μM; 30 min) significantly inhibits NLRP3-mediated IL-1β release in human PBMCs, acting as a specific NLRP3 inhibitor[1].
NT-0527 (5 μM) exhibits high passive permeability and an efflux ratio in Caco-2 monolayer cell model, and is not a substrate for efflux transporters[1].
NT-0527 (1 μM) shows extremely low intrinsic clearance in human liver microsomes and cryopreserved hepatocytes, while moderate to high intrinsic clearance in rat and mouse liver microsomes and cryopreserved hepatocytes, showing the metabolic clearance rate in human liver is much slower than that in rats and mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | MRT | CLplasma | Vss | AUC0-inf | F |
|---|---|---|---|---|---|---|---|
| Cynomolgus Monkey[1] | 3 mg/kg | i.v. | 3.9 h | 6.3 mL/min/kg | 1.4 L/kg | 8200 ng·h/mL | 104 % |
| Cynomolgus Monkey[1] | 3 mg/kg | p.o. | 3.9 h | 6.3 mL/min/kg | 1.4 L/kg | 9700 ng·h/mL | 104 % |
| Mice[1] | 3 mg/kg | i.v. | 0.25 h | 42 mL/min/kg | 0.63 L/kg | 1200 ng·h/mL | 39 % |
| Mice[1] | 3 mg/kg | p.o. | 0.25 h | 42 mL/min/kg | 0.63 L/kg | 470 ng·h/mL | 39 % |
| Pig[1] | 1 mg/kg | i.v. | / | / | / | / | / |
| Pig[1] | 2 mg/kg | p.o. | / | / | / | / | / |
| Rat[1] | 3 mg/kg | i.v. | 0.58 h | 10 mL/min/kg | 0.36 L/kg | 4800 ng·h/mL | 50 % |
| Rat[1] | 3 mg/kg | p.o. | 0.58 h | 10 mL/min/kg | 0.36 L/kg | 2400 ng·h/mL | 50 % |
NT-0527 (10 mg/kg; oral gavage; single administration; 24 h) achieves an almost even distribution between blood and cerebrospinal fluid[1].
NT-0527 (1-100 mg/kg; oral gavage) dose-dependently inhibits peritoneal IL-1β production with significant effect at 10 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male non-naïve cynomolgus monkeys were administered formulated in 0.5% methocel (400cp) and 0.2% Tween 80 in purified water[1].
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Dosage:10 mg/kg
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Administration:Oral gavage (p.o.); single administration; 24 h
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Result:Achieved an almost even distribution between blood and cerebrospinal fluid (CSF), demonstrating efficient central nervous system (CNS) penetration.
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Animal Model:Male SD rats (fed) were subjected to non-recovery anaesthesia and cannulated at the right carotid artery for hemi-brain perfusion[1].
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Dosage:5 μM
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Administration:Carotid artery perfusion; single administration; 0.25-0.5 min
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Result:Exhibited high brain permeability, which was significantly higher than the low-permeability sulfonylurea NLRP3 inhibitors CRID3 (0.09 μM) (HY-12815) and emlenoflast (0.25 μM) (HY-137245); the permeability was higher than the high-permeability control diazepam (4.3 μM).
Chemical Information
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No. CAS 2771019-10-2
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Appearance Solid
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Peso molecular 360.77
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Fòrmula C17H14ClFN4O2
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Color White to off-white
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SMILES
O=C1C2=CC=C(C=C2C3(CC3)CN1CC(NC4=NC=C(C=N4)F)=O)Cl
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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
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
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- Korean - KR (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NT-0527 Related Classifications
HY-186072 Related Classifications
Powered by Bioz
- NT-0527
- 2771019-10-2
- NT0527
- NT 0527
- NOD-like Receptor (NLR)
- Interleukin Related
- Cytochrome P450
- NLRP3 inflammasome inhibitor
- inhibition of IL-1β release
- inhibition of CYP2C19
- human peripheral blood mononuclear cells (PBMCs)
- human whole blood
- Caco-2 monolayer cells
- C57BL/6J mice
- SD rats
- cynomolgus monkeys
- Bama minipigs
- mouse LPS/ATP-induced peritonitis model
- rat in situ brain perfusion model
- cynomolgus monkey CSF exposure model
- Parkinson's disease
- Alzheimer's disease
- amyotrophic lateral sclerosis (ALS)
- type II diabetes
- atherosclerosis
- obesity
- gout
- asthma
- inflammatory bowel disease (IBD)
- Metabolic Disease
- Inhibitor
- inhibitor
- inhibit