2. Immunology/Inflammation Metabolic Enzyme/Protease
  3. NOD-like Receptor (NLR) Interleukin Related Cytochrome P450
  4. NT-0527

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.

For research use only. We do not sell to patients.

NT-0527

NT-0527 Chemical Structure

CAS No. : 2771019-10-2

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Based on 1 publication(s) in Google Scholar

NT-0527 Related Antibodies

Top Publications Citing Use of Products

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NLRP3 NLRP1 NOD1 NOD2

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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Description

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[1].

IC50 & Target[1]

IL-1β

0.79 μM (IC50)

CYP2C19

 

NLRP3 inflammasome

 

In Vitro

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.

NT-0527 Related Antibodies
Parmacokinetics
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 %
In Vivo

NT-0527 (5 μM; carotid artery perfusion; 0.25-0.5 min) exhibits high brain permeability in male SD rat in situ brain perfusion model[1].
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).
Molecular Weight

360.77

Formula

C17H14ClFN4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=CC=C(C=C2C3(CC3)CN1CC(NC4=NC=C(C=N4)F)=O)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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NT-0527 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NT-05272771019-10-2NT0527NT 0527NOD-like Receptor (NLR)Interleukin RelatedCytochrome P450ILCYPsNLRP3 inflammasome inhibitorinhibition of IL-1β releaseinhibition of CYP2C19human peripheral blood mononuclear cells (PBMCs)human whole bloodCaco-2 monolayer cellsC57BL/6J miceSD ratscynomolgus monkeysBama minipigsmouse LPS/ATP-induced peritonitis modelrat in situ brain perfusion modelcynomolgus monkey CSF exposure modelParkinson's diseaseAlzheimer's diseaseamyotrophic lateral sclerosis (ALS)type II diabetesatherosclerosisobesitygoutasthmainflammatory bowel disease (IBD)Metabolic DiseaseInhibitorinhibitorinhibit

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