Ruvonoflast

Ruvonoflast (NT-0796) is an orally active, selective and CNS-penetrant NLRP3 inflammasome inhibitor. Ruvonoflast inhibits IL-1β release in human PBMC cells with an IC50 value of 0.32 nM. Ruvonoflast is an isopropyl ester that undergoes intracellular conversion to Ruvonoflast, the carboxylic acid active species. Ruvonoflast reverses high fat diet-induced obesity, systemic inflammation and astrogliosis in the diet-induced obesity mouse model. Ruvonoflast is promising for research of neurodegenerative disorders, including Alzheimer’s disease, Parkinson’s disease, multiple sclerosis, and amyotrophic lateral sclerosis[1][2][3][4].

Product Specifications

CAS Number

[2272917-13-0]

Product Name Alternative

NT-0796

UNSPSC

12352005

Target

Interleukin Related; NOD-like Receptor (NLR)

Type

Reference compound

Related Pathways

Immunology/Inflammation

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/nt-0796.html

Purity

99.65

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC(C)OC([C@H](OC(NC1=C2C(CCC2)=CC3=C1CCC3)=O)CC4=NC=CC=N4)=O

Molecular Formula

C23H27N3O4

Molecular Weight

409.48

References & Citations

[1]David Harrison, et al. Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders. J Med Chem. 2023 Oct 24.|[2]Thornton P, et al. Reversal of High Fat Diet-Induced Obesity, Systemic Inflammation, and Astrogliosis by the NLRP3 Inflammasome Inhibitors NT-0249 and NT-0796. J Pharmacol Exp Ther. 2024 Feb 15;388 (3) :813-826.|[3]Smolak P, et al. Target Cell Activation of a Structurally Novel NOD-Like Receptor Pyrin Domain-Containing Protein 3 Inhibitor NT-0796 Enhances Potency. J Pharmacol Exp Ther. 2024 Feb 15;388 (3) :798-812. |[4]Doedens JR, et al. The ester-containing prodrug NT-0796 enhances delivery of the NLRP3 inflammasome inhibitor NDT-19795 to monocytic cells expressing carboxylesterase-1. Biochem Pharmacol. 2024 Sep;227:116455.