NLRP3-IN-10

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

NLRP3-IN-10 is a potent NLRP3?inhibitor, inhibits IL-1β release with an IC50 value of 251.1 nM. NLRP3-IN-10 suppresses NLRP3 inflammasome activation by attenuating ASC speck formation.

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.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.

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 (14.6?23.53 μg·h/L), poor bioavailability (2.47?13.79%), and high plasma clearance (2201.58?5551.12 L/h/kg) after different doses for oral administration.Animal Model: MSU-induced peritonitis in a LPS-primed mouse model (C57BL/6J mice, 7-week-old, male) LPS: 1 mg/kg, i.p.; MSU: 100 mg/kg, i.v.Dosage:10 mg/kg Administration:Intravenous injection; single dose Result: Significantly reduced IL-1β release in the spleen of mice after 6 h treatment.Significantly reduced the increase of peritoneal neutrophil influx compared with the control group.

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NF-κB

NOD

NOD

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2641826-39-1

365.19

C17H14BrFO3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (273.83 mM; 超声助溶 )

COc1cc(\C=C\C(=O)c2ccc(F)cc2)c(OC)cc1Br

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(-20℃)

With Ice Pack

≥ 2 years