货号	规格	价格	上海	北京	珠海	重庆	武汉
S89876-5mg买3赠1	99.90%	￥395.00 S89876-5mg ￥395.00 现货（买3赠1）	5 5	-	-	-	-
S89876-10mg买3赠1	99.90%	￥660.00 S89876-10mg ￥660.00 现货（买3赠1）	8 8	-	-	-	-
S89876-25mg促销	99.90%	￥1330.00 ￥1060.00 S89876-25mg ￥1060.00 现货	5 5	-	-	-	-
S89876-100mg促销	≥98%	￥3300.00 ￥2640.00 S89876-100mg ￥2640.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

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。

靶点：

NLRP3：251.1 nM (IC50);NOD

体外研究：

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.

体内研究：

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.

参考文献：

1. Zhang R, et al. New Highly Potent NLRP3 Inhibitors: Furanochalcone Velutone F Analogues. ACS Med Chem Lett. 2022 Mar 7;13(4):560-569.

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.738 ml	13.692 ml	27.383 ml
5 mM	0.548 ml	2.738 ml	5.477 ml
10 mM	0.274 ml	1.369 ml	2.738 ml
50 mM	0.055 ml	0.274 ml	0.548 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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