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NIC-0102

目录号 : GC71149

NIC-0102是一种口服活性蛋白酶体抑制剂(pIC50=7.55),其特异性抑制NLRP3炎性囊泡激活。

NIC-0102 Chemical Structure

Cas No.:2806031-94-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,418.00
现货
1 mg
¥1,044.00
现货
5 mg
¥2,628.00
现货
10 mg
¥4,464.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β.

NIC-0102 (compound 27) (7.5, 15, 30, 60 nM; 1h) specifically suppresses NLRP3 inflammasome activation in LPS-primed J774A.1 and BMDM cells[1].
NIC-0102 (7.5, 15, 30, 60 nM; 1h) induces polyubiquitination of NLRP3 via inhibition of the proteasome during the activation step in LPS-primed J774A.1 cells[1].
NIC-0102 (7.5, 15, 30, 60 nM; 1h) exhibits inhibitory effects on NF-κB in the priming step of the NLRP3 pathway in LPS-primed J774A.1 cells[1].
NIC-0102 (15, 60 nM; 1h) blocks NLRP3-ASC interaction and ASC oligomerization in LPS-primed J774A.1 cells[1].

NIC-0102 (0.125, 0.25, 0.5 mg/kg; p.o.; single every 72 h for 10 days) shows strong protection against DSS-induced acute colitis in mice[1].

References:
[1]. Wu X, et al. Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity. J Med Chem. 2022 Sep 5.

Chemical Properties

Cas No. 2806031-94-5 SDF
分子式 C21H25BF2N2O4 分子量 418.24
溶解度 DMSO : 100 mg/mL (239.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 储存条件 -20°C
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1 mg 5 mg 10 mg
1 mM 2.391 mL 11.9549 mL 23.9097 mL
5 mM 0.4782 mL 2.391 mL 4.7819 mL
10 mM 0.2391 mL 1.1955 mL 2.391 mL
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