NLRP3-IN-9

Names

[ Name ]:
NLRP3-IN-9

Biological Activity

[Description]:

NLRP3-IN-9 is a potent NLRP3 inhibitor. NLRP3-IN-9 inhibits IL-1β release. NLRP3-IN-9 reduces inflammation and mechanical hyperalgesia. NLRP3-IN-9 has the potential for the research of gout[1].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> NOD-like Receptor (NLR)

Research Areas >> Inflammation/Immunology

[Target]

NLRP3

[In Vitro]

NLRP3-IN-9 (compound 4b) (0.01-3 µM) 在 ATP (5 mM) 和 LPS (1 µg/mL) 诱导的巨噬细胞中以剂量依赖性方式抑制 IL-1β 释放[1]< /sup>. NLRP3-IN-9 (1 µM; 15 min) 抑制 NLRP3 炎性体寡聚化[1]。 Western Blot Analysis[1] Cell Line: Macrophages Concentration: 1 µM Incubation Time: 15 min Result: Inhibited teh expression of IL-1β P17, Casp-1 p10 peotein levelwith the ATP (5 mM) and LPS (1 µg/mL)-induced in the supernatant of the cultures, without affecting the intracellular levels of their precursors.

[In Vivo]

NLRP3-IN-9 (3, 10 mg/kg; i.p.) 减少急性痛风小鼠模型中的炎症和机械痛觉[1]。 Animal Model: 3-4 month old male and female C57BL/6J WT and NLRP3-KO mice[1] Dosage: 3, 10 mg/kg Administration: I.p. Result: Reduced paw swelling by 40% in males and 33% in females at 3 mg/kg, and 66% in males and 52% in females at 10 mg/kg in WT mouse.

[References]

[1]. Narros-Fernández P, et al. Synthesis and Pharmacological Evaluation of New N-Sulfonylureas as NLRP3 Inflammasome Inhibitors: Identification of a Hit Compound to Treat Gout. J Med Chem. 2022 Apr 28;65(8):6250-6260.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₆H₁₉N₂NaO₅S

[ Molecular Weight ]:
374.39

Related Compounds

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