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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.80%
- CAS No.: 2771019-10-2
- 화학식: C17H14ClFN4O2
- 분자량:360.77
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
NF-κB Signaling Compound Library
HY-L014
-
CNS-Penetrant Compound Library
HY-L028
-
Anti-Aging Compound Library
HY-L034
-
Antioxidant Compound Library
HY-L037
-
Anti-diabetic Compound Library
HY-L040
-
Oxygen Sensing Compound Library
HY-L045
-
Pyroptosis Compound Library
HY-L059
-
Orally Active Compound Library
HY-L061
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Anti-Parkinson's Disease Compound Library
HY-L085
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Angiogenesis-Related Compound Library
HY-L088
-
Mitochondria-Targeted Compound Library
HY-L089
-
Antidepressant Compound Library
HY-L108
-
Pain-Related Compound Library
HY-L139
-
Metabolic Enzyme Compound Library
HY-L146
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Autoimmune Disease Compound Library
HY-L156
-
Highly Selective Inhibitors Library
HY-L158
-
Inflammasomes related Compound Library
HY-L175
-
Multi-Target Compound Library
HY-L176
-
Radioprotector Library
HY-L178
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Pattern Recognition Receptors Library
HY-L237
Biological Activity
|
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.
-
Animal Model:Male non-naïve cynomolgus monkeys were administered formulated in 0.5% methocel (400cp) and 0.2% Tween 80 in purified water[1].
-
Dosage:10 mg/kg
-
Administration:Oral gavage (p.o.); single administration; 24 h
-
Result:Achieved an almost even distribution between blood and cerebrospinal fluid (CSF), demonstrating efficient central nervous system (CNS) penetration.
-
Animal Model:Male SD rats (fed) were subjected to non-recovery anaesthesia and cannulated at the right carotid artery for hemi-brain perfusion[1].
-
Dosage:5 μM
-
Administration:Carotid artery perfusion; single administration; 0.25-0.5 min
-
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
-
CAS No. 2771019-10-2
-
Appearance Solid
-
분자량 360.77
-
화학식 C17H14ClFN4O2
-
Color White to off-white
-
SMILES
O=C1C2=CC=C(C=C2C3(CC3)CN1CC(NC4=NC=C(C=N4)F)=O)Cl
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
순도&문서
-
Data Sheet (272 KB)
-
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)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
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