2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. NLRP3-IN-12

NLRP3-IN-12 是一种特异性的 NLRP3 炎症小体抑制剂。NLRP3-IN-12 通过靶向 NLRP3 蛋白抑制 IL-1β 的释放，IC50 值为 0.45 μM。NLRP3-IN-12 可用于研究炎症性肠病。

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NLRP3-IN-12 Chemical Structure

NLRP3-IN-12 Chemical Structure

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NLRP3-IN-12 相关抗体

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查看 NOD-like Receptor (NLR) 亚型特异性产品:

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NLRP3 NLRP1 NOD1 NOD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NLRP3-IN-12 is a specific NLRP3 inflammasome inhibitor. NLRP3-IN-12 reduces the release of IL-1β by targeting the NLRP3 protein, with an IC50 of 0.45 μM. NLRP3-IN-12 can be used for the research of inflammatory bowel disease[1].

IC50 & Target

NLRP3 inflammasome[1]
体外研究
(In Vitro)

NLRP3-IN-12 (化合物 6E) (0.5-2 μM; 预处理 1 h) 抑制 THP-M 细胞中 LPS/ATP 刺激的裂解 caspase-1 和 IL-1β 的表达[1]。
NLRP3-IN-12 (2 μM) 抑制 THP-M 细胞中的 GSDMD 介导的凋亡[1]。
NLRP3-IN-12 (1 μM) 在人和大鼠肝微粒体中的半衰期 (T1/2) 分别为 53.4 min 和 31.8 min[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NLRP3-IN-12 相关抗体:

Western Blot Analysis[1]

Cell Line: THP-M cells
Concentration: 0.5, 1, 2 μM
Incubation Time: Pretreated for 1 h, then stimulated with LPS (1 μg/mL) for 4.5 h, and ATP (5 mM) for 0.5 h.
Result: Reduced the secretion of IL-1β and caspase-1.
Had no effect on the levels of NLRP3, pro-IL-1β, ASC, pro-caspase 1, p65, p-p65, IκBα, and p-IκBα.
体内研究
(In Vivo)

NLRP3-IN-12 (化合物 6E) (5-10 mg/kg; i.p. daily for 10 d) 减弱小鼠 DSS 诱导的结肠炎[1]。
NLRP3-IN-12 (20 mg/kg; i.v.) 在大鼠体内半衰期 (T1/2) 为 6.64 h，消除速率常数 (Kel) 为 0.107 h，清除率 (CL) 为 105 mL/kg/min，稳态的表观分布体积 (Vdss) 为 23.1 L/kg[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice were induced acute colitis by drinking 3% DSS (dextran sulfate sodium)[1]
Dosage: 5, 10 mg/kg
Administration: Intraperitoneal injection daily for 10 days in aqueous solution containing DMSO/0.5% CMC-Na/normal saline
Result: Attenuated DSS-induced weight loss, loose stools, bloody stools, shortened colons, increased disease activity index score, and lower survival rate.
分子量

518.00

Formula

C27H32ClNO7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NLRP3-IN-12 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NLRP3-IN-12NOD-like Receptor (NLR)inflammasomeIL-1βinflammatory bowel diseaseInhibitorinhibitorinhibit

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