2. Immunology/Inflammation NF-κB
  3. NOD-like Receptor (NLR) Interleukin Related NF-κB
  4. NLRP3-IN-75

NLRP3-IN-75 是一种口服有效的 NLRP3 抑制剂。NLRP3-IN-75 可抑制 IL-1β 的分泌 (IC50 = 23 nM)。NLRP3-IN-75 通过破坏炎症小体的组装选择性抑制 NLRP3 活化，但不影响 NLRC4 或 AIM2 炎症小体的组装。NLRP3-IN-75 在急性腹膜炎、糖尿病肾病和炎症性肠病 (IBD) 等模型中表现出优异的抗炎效果。

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NLRP3-IN-75

NLRP3-IN-75 Chemical Structure

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NLRP3-IN-75 相关抗体

Top Publications Citing Use of Products

查看 NOD-like Receptor (NLR) 亚型特异性产品:

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NLRP3 NLRP1 NOD1 NOD2

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NLRP3-IN-75 is an orally active NLRP3 inhibitor. NLRP3-IN-75 suppresses IL-1β secretion (IC50 = 23 nM). NLRP3-IN-75 selectively inhibits NLRP3 activation by disrupting inflammasome assembly without affecting NLRC4 or AIM2 inflammasomes. NLRP3-IN-75 exhibits superior efficacy in acute peritonitis, diabetic kidney disease and IBD models[1].

IC50 & Target

IL-1β

23 nM (IC50)

体外研究
(In Vitro)

NLRP3-IN-75 (Compound 15) (0.03-100 μM，30 分钟) 显著抑制 LPS 和 ATP 诱导的 BMDM 细胞 (IC50 = 0.106 μM) 和 THP-1 细胞 (IC50 = 23 nM) 中 IL-1β 的释放[1]。
NLRP3-IN-75 (10 μM，4 小时) 通过在鞭毛蛋白转染的 BMDM 细胞中维持 NLRC4 或 AIM2 炎症小体通路中的 IL-1β 分泌，显示出对 NLRP3 炎症小体的选择性[1]。
NLRP3-IN-75 (10 μM，4 小时) 不会影响 NLRP3 炎症激活的起始阶段，因为不会影响 TNF-α 和 IL-6 的产生[1]。
NLRP3-IN-75 (10 μM，4 小时) 通过阻碍 NLRP3 炎症小体的组装，阻断 BMDM 细胞中 LPS 和 ATP 诱导的 NLRP3 与 ASC 之间的相互作用[1]。

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

NLRP3-IN-75 相关抗体:
药代动力学
(Parmacokinetics)[1]
Species Dose SampleTime Route Indicator value
Mice 20 mg/kg 1 h p.o. AUC0-t 57916 ng·h/mL
Mice 5 mg/kg 1 h i.v. AUC0-t 14525 ng·h/mL
Mice 20 mg/kg 1 h p.o. F 99.6 %
Mice 5 mg/kg 1 h i.v. T1/2 3.63 hr
Mice 20 mg/kg 1 h p.o. T1/2 2.70 hr
Mice 20 mg/kg 1 h p.o. Tmax 0.33 hr
体内研究
(In Vivo)

NLRP3-IN-75 (20 mg/kg，口服，单次给药) 可改善小鼠模型中 LPS 和 ATP 诱导的急性腹膜炎[1]。
NLRP3-IN-75 (20 mg/kg，口服，6周) 通过靶向 NLRP3 炎症小体，减轻小鼠 HFD 和 STZ 诱导的 DKD[1]。
NLRP3-IN-75 (0.2-5 mg/kg，口服，10 天) 可改善小鼠模型中 DSS (HY-116282C) 诱发的炎症性肠病[1]。
NLRP3-IN-75 (20 mg/kg，口服，单次给药) 对小鼠心血管或肺部毒性较低[1]。

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

Animal Model: LPS (HY-D1056) (15 mg/kg, i.p.)- and ATP (1 mM/kg, i.p.)-induced acute peritonitis mice (6-8 weeks old, male C57BL/6J)[1]
Dosage: 1 mg/kg, 20 mg/kg
Administration: Oral gavage (p.o.)
Result: Achieved 100% survival rate in LPS-induced followed by ATP-induced acute peritonitis mice models.
Suppressed serum IL-1β level in peritonitis mice models 12 h post-ATP administration, and presented better effect with increasing dose.
Animal Model: Male C57BL/6J HFD (4 weeks)- and STZ (HY-13753) (50 mg/kg, i.p., 5 days)-induced diabetic kidney disease (DKD) mice (n = 5-6, 20-22 g)[1]
Dosage: 20 mg/kg, 6 weeks
Administration: Oral gavage (p.o.), 6 weeks; administered after STZ and HFD feeding
Result: Significantly reduced the elevated urine albumin-to-creatinine ratio (UACR) caused by the HFD- and STZ-induced DKD mice models.
Ameliorated the thickening of the glomerular and tubular basement membranes in DKD models.
Decreased inflammatory cytokine IL-1β but no effect on TNF-α level[1].
Reduced macrophage infiltration.
Disrupted the NLRP3-ASC interaction.
Reduced LDL-C levels without affecting HDL-C levels.
Animal Model: 2% (w/v) DSS (HY-116282C) (7 days) in distilled water-induced colitis mice (Male C57BL/6J, n = 5-10, 20-22 g)[1]
Dosage: 0.2 or 5 mg/kg
Administration: Oral gavage (p.o.) , 9 days (day 1-day 10)
Result: Attenuated weight loss in DSS-induced acute colitis mice models.
Reduced fecal bleeding and decreased disease activity index (DAI) scores.
Ameliorated pathological features such as disruption of mucosal barrier, crypt necrosis, substantial depletion of the mucosal barrier, crypt necrosis, substantial depletion of goblet cells, and pronounced infiltration of inflammatory cells.
Inhibited colonic IL-1β without affecting TNF-α level.
分子量

406.54

Formula

C20H30N4O3S
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-75 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-75NOD-like Receptor (NLR)Interleukin RelatedNF-κBILNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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