YQ128,2454246-18-3

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YQ128

CAS No. : 2454246-18-3

MCE 国际站：YQ128

产品活性：YQ128 是有效的，选择性第二代 NLRP3 炎性体抑制剂，IC₅₀ 为 0.30 μM。YQ128 能显着和选择性地抑制 IL-1β 的产生，但不抑制 TNF-α 的产生。YQ128 可以穿过血脑屏障到达中枢神经系统。YQ128 具有抗炎活性。YQ128 是一种点击化学试剂。它含有 Alkyne 基团，可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

研究领域：Immunology/Inflammation

作用靶点：NOD-like Receptor (NLR)  |  Interleukin Related

In Vitro: YQ128 (0.3-100 µM; 30 mins) dose dependently suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC₅₀ of 1.59 µM.
YQ128 (20 µM; 2 hours) shows no significant toxic effects on hCMEC/D3 cells.

In Vivo: YQ128 (iv; 20 mg/kg) has an intermediate terminal plasma half-life (t_1/2) of 6.6 hours after iv administration.
YQ128 (oral; 20 mg/kg) shows delayed gastrointestinal absorption with a t_max and c_max of 12 h and 73 ng/mL, respectively. Oral bioavailability (F_oral) is estimated as 10%.
YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vd_ss) of 8.5 L/kg and rapid total clearance (CL_tot) of 41 mL/min/kg.
YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner in C57BL/6 mice.

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