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YQ128

Catalog No. T13375 CAS 2454246-18-3

YQ128 is a potent and selective inhibitor of second-generation NLRP3 (NOD-like receptor P3) inflammasome(IC50 of 0.30 µM), with anti-inflammatory activity.

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YQ128, CAS 2454246-18-3

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	YQ128 is a potent and selective inhibitor of second-generation NLRP3 (NOD-like receptor P3) inflammasome(IC50 of 0.30 µM), with anti-inflammatory activity.
Targets&IC50	NLRP3:0.30 μM, IL-1β:
In vitro	The release of IL-1β from peritoneal macrophages upon LPS/ATP challenge(IC50 of 1.59 μM) dose dependently suppressed by YQ128 (0.3-100 μM; 30 mins).
In vivo	YQ128 (oral; 20 mg/kg) shows delayed gastrointestinal absorption with a tmax and cmax of 12 h and 73 ng/mL, respectively. YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vdss) of 8.5 L/kg and rapid total clearance (CLtot) of 41 mL/min/kg. In C57BL/6 mice, YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner .

Molecular Weight	545.11
Formula	C27H29ClN2O4S2
CAS No.	2454246-18-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 248 mg/mL (454.95 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. 1.Jiang Y, et al. Discovery of Second-Generation NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization. J Med Chem. 2019 Oct 31.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

YQ128 2454246-18-3 NF-Kb信号通路免疫与炎症 IL Receptor Interleukin NOD NOD-like Receptor (NLR) inhibit YQ 128 Inhibitor Interleukin Related YQ-128 inhibitor

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