GDC-2394

GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC50s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β) . GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation[1][2].

Product Specifications

CAS Number

[2238822-07-4]

UNSPSC

12352005

Target

Caspase; Interleukin Related; NOD-like Receptor (NLR)

Type

Reference compound

Related Pathways

Apoptosis; Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/gdc-2394.html

Purity

99.87

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=S(C1=C2OC[C@@H](NC)CN2N=C1)(NC(NC3=C4CCCC4=CC5=C3CCC5)=O)=O

Molecular Formula

C20H25N5O4S

Molecular Weight

431.51

References & Citations

[1]McBride C, et al. Overcoming Preclinical Safety Obstacles to Discover (S) -N- ((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl) carbamoyl) -6- (methylamino) -6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394) : A Potent and Selective NLRP3 Inhibitor. J Med Chem. 2022 Oct 24. |[2]Stafford, et al. Preparation of hexahydroindacenylcarbamoyldihydropyrazolooxazinesulfonamide derivatives and analogs for use as interleukin-1 activity inhibitors: World Intellectual Property Organization, WO2018136890[P]. 2018-07-26.