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NLRP3-IN-10

Catalog No. T61392 CAS 2641826-39-1

Synonyms: ZVN26391

NLRP3-IN-10 (ZVN26391) is a potent NLRP3 inhibitor. NLRP3-IN-10 inhibits IL-1β release with an IC50 value of 251.1 nM. NLRP3-IN-10 attenuates ASC speck formation, leading to suppress activation of NLRP3 inflammasome.

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NLRP3-IN-10, CAS 2641826-39-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 64.00
25 mg	In stock	$ 128.00
50 mg	In stock	$ 197.00
100 mg	In stock	$ 328.00
200 mg	In stock	$ 489.00
1 mL * 10 mM (in DMSO)	In stock	$ 59.00

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Purity: 99.63%

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Description	NLRP3-IN-10 (ZVN26391) is a potent NLRP3 inhibitor. NLRP3-IN-10 inhibits IL-1β release with an IC50 value of 251.1 nM. NLRP3-IN-10 attenuates ASC speck formation, leading to suppress activation of NLRP3 inflammasome.
In vitro	NLRP3-IN-10 (compound 14c) demonstrates significant inhibitory effects on the activation of the NLRP3 inflammasome in THP-1 cells by LPS-MSU, showing a dose-dependent effectiveness with concentrations between 0.4 and 6.4 μM over 40 minutes. It is non-toxic to THP-1 cells across a range of 0.1 to 6.4 μM after 1.5 hours of exposure, and at concentrations of 0.1 and 0.4 μM, it prevents Nigericin-induced pyroptosis. Additionally, it decreases the production of caspase-1 p20 and IL-1β in a dose-dependent manner at concentrations of 0.1, 0.2, and 0.4 μM. At higher concentrations, 3 and 5 μM, NLRP3-IN-10 reduces LPS-induced TNF-α production, and at 0.2 and 0.8 μM, it diminishes the occurrence of ASC specks in THP-1 cells, suggesting it interrupts ASC oligomerization. Moreover, it effectively inhibits LPS-induced NLRP3 priming by directly interacting with NLRP3 at concentrations of 1, 10, and 100 μM, highlighting its potential in managing two key steps in the NLRP3 inflammasome pathway: priming and activation.
In vivo	NLRP3-IN-10 (compound 14c), administered via a single intravenous (i.v.) dose of 10 mg/kg, effectively reduced peritoneal neutrophil influx and IL-1β levels in the spleen in a LPS-primed mouse model with MSU-induced peritonitis. Additionally, oral administration of NLRP3-IN-10 at doses of 10, 30, and 90 mg/kg demonstrated very low systemic exposure (14.6 to 23.53 μg·h/L), limited bioavailability (2.47 to 13.79%), and high plasma clearance rates (2201.58 to 5551.12 L/h/kg), indicating significant challenges in its pharmacokinetic profile when administered orally. Pharmacokinetic data revealed an area under the curve (AUC) ranging from 14.60 to 23.53 μg·h/L, clearance (CL) rates between 2201.58 and 5551.12 L/h/kg, and maximal concentration (Cmax) values from 3.35 to 81.97 μg/L across different administration routes and dosages. The study was conducted on 7-week-old male C57BL/6J mice induced with MSU-induced peritonitis and primed with LPS (1 mg/kg, i.p.), showing a notable reduction in spleen IL-1β release and peritoneal neutrophil influx following a 6-hour treatment with a 10 mg/kg intravenous dose of NLRP3-IN-10, when compared to the control group.

Synonyms	ZVN26391
Molecular Weight	365.19
Formula	C17H14BrFO3
CAS No.	2641826-39-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.4 mg/mL (12.05 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Compound Library NF-κB Signaling Compound Library Bioactive Compound Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library

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Keywords

NLRP3-IN-10 2641826-39-1 Immunology/Inflammation NF-Κb NOD ZVN26391 ZVN 26391 ZVN-26391 inhibitor inhibit

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