GDC-2394 (GDC2394) | NLRP3 inhibitor | Probechem Biochemicals

Chemical Structure : GDC-2394

CAS No.: 2238822-07-4

GDC-2394 (GDC2394, GDC 2394)

Catalog No.: PC-49396Not For Human Use, Lab Use Only.

GDC-2394 (GDC2394) is a potent and selective NLRP3 inhibitor with IC50 of 5.4 nM (IL-1β inhibition in PBMCs).

Packing	Price	Stock
2 mg	$158	In stock
5 mg	$278	In stock
10 mg	$478	In stock
25 mg	$798	In stock
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Biological Activity

GDC-2394 (GDC2394) is a potent and selective NLRP3 inhibitor with IC50 of 5.4 nM (IL-1β inhibition in PBMCs).

GDC-2394 inhibits NLRP3-induced caspase-1 activity with IC50 of 51 nM in in THP1 cells, but does not inhibit NLRC4-dependent inflammasome activation.

GDC-2394 inhibits NLRP3-dependent IL-1β release from mouse bone marrow-derived macrophages (BMDMs) with IC50 of 63 nM.

GDC-2394 inhibits LPS plus nigericin-induced ASC speck formation in THP-1 cells with IC50 of 48 nM.

GDC-2394 inhibits production of IL-1β in human and mouse WB in response to LPS priming and activation by ATP, and also LPS priming and activation by MSU crystals, calcium pyrophosphate dehydrate, and cholesterol crystals in HWB and macrophages.

GDC-2394 (25 mg/kg) significantly reduces joint swelling and pain scores, comparable to that achieved by IL-1β blockade, in rodent model of gouty arthritis induced by intra-articular injection of MSU crystals.

Physicochemical Properties

M.Wt	431.511
Formula	C20H25N5O4S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(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

References

1. Christopher McBride, et al. J Med Chem. 2022 Oct 24. doi: 10.1021/acs.jmedchem.2c01250.

GDC-2394 (GDC2394, GDC 2394)

Biological Activity

Physicochemical Properties

References

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