VEN-02XX

Chemical Structure : VEN-02XX

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货号: PC-24562Not For Human Use, Lab Use Only.

VEN-02XX is a a novel potent and selective brain-penetrant small molecule NLRP3 inhibitor with binding KD of 93.3 nM, inhibits IL-1β production in PBMCs with IC50 of 0.35 uM.

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生物&药学活性

VEN-02XX is a a novel potent and selective brain-penetrant small molecule NLRP3 inhibitor with binding KD of 93.3 nM, inhibits IL-1β production in PBMCs with IC50 of 0.35 uM.
VEN-02XX induces NLRP3 inhibition in various cellular systems with sub-micromolar potency including peripheral blood mononuclear cell (PBMC), iPSC-derived microglia and whole blood.
VEN-02XX is lack of TNFα inhibition in cellular assay, also does not block IL-1β release downstream of other inflammasomes like absent in melanoma 2 (AIM2), NOD-like-receptor containing a Pyrin domain 1 (NLRP1) and the NLR-family CARD domain-containing protein 4 (NLRC4).
VEN-02XX significantly reduced microgliosis and neuroinflammation, limited neurodegeneration, and dramatically improved memory and cognition in a dose-dependent manner.
VEN-02XX (20 mg/kg) treatment improved MAP2 levels in the 5xFAD/Rubicon KO mice.

物理化学性质&存储条件

分子量	396.80
分子式	C18H16ClF3N4O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-((1-(4-chloro-2-(trifluoromethyl)phenyl)pyrido[3,4-d]pyridazin-4-yl)amino)-2-methylpropan-2-ol

参考文献

1. Auger A, et al. NPJ Dement. 2025;1(1):3.

VEN-02XX

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VEN-02XX

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