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NLRP3-IN-10

CAS No. : 2641826-39-1

MCE 站：NLRP3-IN-10

产品活性：NLRP3-IN-10 是一种强效的 NLRP3 抑制剂，抑制 IL-1β 的 IC₅₀ 为 251.1 nM。NLRP3-IN-10 能够减弱ASC斑点形成抑制NLRP3炎症小体激活。

研究领域：Immunology/Inflammation

作用靶点：NOD-like Receptor (NLR)

In Vitro: NLRP3-IN-10 (compound 14c) (0.4, 1.6, 6.4 μM; 40 min) exerts remarkable inhibitory activity on NLRP3 inflammasome activation induced by LPS-MSU (12 h) in THP-1 cells in a dose-dependent manner.
NLRP3-IN-10 (0.1-6.4 μM; 1.5 h) shows no cytotoxicity against THP-1 cells ａnd (0.1, ａnd 0.4 μM; 40 min) avoids Nigericin (HY-127019)-induced pyroptosis.
NLRP3-IN-10 (0.1, 0.2, ａnd 0.4 μM; 40 min) reduces the processing of caspase-1 p20 ａnd IL-1β, in supernatants in THP-1 cells in a dose-dependent manner.
NLRP3-IN-10 (3 μM ａnd 5 μM; 40 min) decreases LPS-induced THF-α, ａnd (0.2 μM ａnd 0.8 μM; 40 min) reduces the rate of THP-1 cells with ASC specks, indicating ASC oligomerization interruptionsup>[1].
NLRP3 inflammasome is regarded as a two-step process, including priming ａnd action. NLRP3-IN-10 (1, 10, ａnd 100 μM; 40 min) suppresses LPS-induced NLRP3 priming through directly interacting with NLRP3.

In Vivo: NLRP3-IN-10 (compound 14c) (10 mg/kg; i.v.; single dose) reduces peritoneal neutrophil influx in mice ａnd IL-1β in the spleen in the MSU-induced peritonitis in LPS-primed mouse model.
NLRP3-IN-10 (10, 30, 90 mg/kg; p.o.; single dose) exhibits extremely low exposure (14.623.53 μgh/L), poor bioavailability (2.4713.79%), ａnd high plasma clearance (2201.585551.12 L/h/kg) after different doses for oral administration.
Pharmacokinetics of NLRP3-IN-10 in mouse

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