2. Immunology/Inflammation Apoptosis
  3. NOD-like Receptor (NLR) Caspase Interleukin Related
  4. 1,2,4-Trimethoxybenzene

1,2,4-Trimethoxybenzene  (Synonyms: 羟基氢醌三甲醚)

目录号: HY-W017087
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1,2,4-Trimethoxybenzene 是一种口服有效的 NLRP3 选择性抑制剂。1,2,4-Trimethoxybenzene 可显著抑制 Nigericin (HY-127019) 或 ATP (HY-B2176) 诱导的 NLRP3 炎症小体活化，从而降低 caspase-1 活化和 IL-1β 分泌。1,2,4-Trimethoxybenzene 特异性抑制 NLRP3 炎症小体的活化，而不影响黑色素瘤缺失 2 (AIM2) 炎症小体的活化。1,2,4-Trimethoxybenzene 抑制凋亡相关斑点样蛋白 (ASC) 的寡聚化以及 NLRP3 与 ASC 之间的蛋白-蛋白相互作用，从而阻断 NLRP3 炎症小体的组装。1,2,4-Trimethoxybenzene 可用于研究实验性自身免疫性脑脊髓炎 (EAE)，多发性硬化症和 2 型糖尿病。

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1,2,4-Trimethoxybenzene

1,2,4-Trimethoxybenzene Chemical Structure

CAS No. : 135-77-3

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1,2,4-Trimethoxybenzene 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

1,2,4-Trimethoxybenzene is an orally active NLRP3 selective inhibitor. 1,2,4-Trimethoxybenzene can markedly suppress Nigericin (HY-127019) or ATP (HY-B2176)-induced NLRP3 inflammasome activation, thus decreasing caspase-1 activation and IL-1β secretion. 1,2,4-Trimethoxybenzene specifically inhibits the activation of NLRP3 inflammasome without affecting absent in melanoma 2 (AIM2) inflammasome activation. 1,2,4-Trimethoxybenzene inhibits oligomerization of the apoptosis-associated speck-like protein containing a CARD (ASC) and protein-protein interaction between NLRP3 and ASC, thus blocking NLRP3 inflammasome assembly. 1,2,4-Trimethoxybenzene can be used for the study of experimental autoimmune encephalomyelitis (EAE), multiple sclerosis, and type 2 diabetes[1][2][3].

IC50 & Target[1]

NLRP3

 

Caspase-1

 

IL-1β

 

体外研究
(In Vitro)

1,2,4-Trimethoxybenzene (0.5-1 mM，1.5 h) 显著抑制 Nigericin 和 Lipopolysaccharides (HY-D1056) (LPS) 诱导的永生化小鼠骨髓来源巨噬细胞 (iBMDM) 中 NLRP3 炎症小体的激活，表现为 caspase-1 (Casp-1) 裂解和 IL-1β 分泌减少[1]。
1,2,4-Trimethoxybenzene (1 mM，75-90 分钟) 抑制 LPS 和 ATP 诱导的 iBMDM、原代小胶质细胞和原代巨噬细胞中 NLRP3 的激活[1]。
1,2,4-Trimethoxybenzene (45 分钟-2 小时) 不抑制 LPS 和 poly(dA:dT) 诱导的原代腹腔巨噬细胞和 Ibmdm 中 AIM2 炎症小体的激活[1]。
1,2,4-Trimethoxybenzene (1小时) 可减少 LPS 和 Nigericin 诱导的 iBMDM 和原代小胶质细胞中 ASC 斑点的形成：免疫荧光显示 ASC 斑点数量显著减少；DSS 交联实验显示可溶性 ASC 增加，不溶性 ASC 减少[1]。
1,2,4-Trimethoxybenzene (1小时) 可阻断 LPS 诱导的 iBMDM 中 NLRP3 与 ASC 之间的蛋白-蛋白相互作用[1]。
1,2,4-Trimethoxybenzene (1 小时) 抑制 LPS 和 Nigericin 诱导的 iBMDM 和原代巨噬细胞的 NLRP3 寡聚化：DSS 交联实验表明 NLRP3 单体、二聚体和更高寡聚体的形成减少[1]。

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

1,2,4-Trimethoxybenzene 相关抗体:

Western Blot Analysis[1]

Cell Line: Immortalized murine bone marrow-derived macrophages (iBMDMs)
Concentration: 0.5 mM, 1 mM
Incubation Time: 1.5 h
Result: Caspase-1 (Casp-1) cleavage and IL-1β secretion are reduced.
体内研究
(In Vivo)

1,2,4-Trimethoxybenzene (200 mg/kg，口服，每日一次，持续 17 天) 可显著缓解 EAE 模型小鼠的临床症状、体重减轻和脱髓鞘病理[1]。
1,2,4-Trimethoxybenzene (50-100 mg/kg，口服，每日一次，连续 3 天) 可通过抑制 NLRP3 炎症小体，增强小鼠恐惧记忆的消退，并缓解创伤后应激障碍 (PTSD) 相关的焦虑和抑郁样行为[2]。
1,2,4-Trimethoxybenzene (50-200 mg/kg，口服，每日一次，连续 8 周) 可通过抑制 NLRP3 炎症小体的激活和调节 2 型糖尿病大鼠的肠道菌群，改善相关的认知功能障碍[3]。

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

Animal Model: Female C57BL/6 mice (6-8 weeks old) were subcutaneously injected with 150 μg of MOG35-55 peptide, and intraperitoneally injected with 200 ng of pertussis toxin on the day of immunization (day 0) and day 2, to simulate EAE[1].
Dosage: 200 mg/kg
Administration: P.o., once daily for 17 days
Result: The incidence of end-stage renal disease (ESRD) decreased, and clinical symptoms were significantly alleviated.
Significantly reduced weight loss indicates a reduction in systemic inflammatory response.
The area of myelin basic protein (MBP) positive in spinal cord sections was significantly larger than in the control group, indicating a reduced degree of demyelination.
The percentage of demyelinated area was significantly lower than in the control group, confirming the protection of myelin structure.
ASC specks were significantly reduced in spinal cord sections, suggesting that NLRP3 inflammasome activation was inhibited.
The expression of NLRP3, ASC, and cleaved caspase-1 proteins was downregulated in spinal cord tissue.
The mRNA expression of pro-inflammatory cytokines IFN-γ and IL-17a and the chemokine CCL-5 was decreased in the spinal cord, while the expression of the anti-inflammatory cytokine IL-4 was upregulated.
Animal Model: Male C57BL/6 mice (8 weeks old) were intraperitoneally injected with lipopolysaccharide (LPS, 2 mg/kg/d) for 3 consecutive days to induce depressive-like behavior[2].
Dosage: 50 mg/kg, 100 mg/kg
Administration: P.o., once daily for 3 days
Result: Sucrose preference was significantly increased (with improved depressive-like behavior), and immobility time in the tail suspension test (TST) and forced swimming test (FST) was significantly reduced.
Activation of the hippocampal NLRP3 inflammasome was inhibited (e.g., reduced expression of cleaved IL-1β, cleaved caspase-1, and ASC spot formation).
Animal Model: Male Sprague-Dawley rats (8 weeks old, 200 g) were first given a high-sugar, high-fat diet for 5 weeks, and then type 2 diabetes (T2DM) was induced by intraperitoneal injection of streptozotocin (STZ, 30 mg/kg)[3].
Dosage: 50 mg/kg, 100 mg/kg, 200 mg/kg
Administration: P.o., once daily for 8 weeks
Result: Significant improvements were observed in blood glucose levels (FBG, OGTT-AUC), insulin resistance index (HOMA-IR), and blood lipids (TC, TG, LDL-C) in rats, along with a decrease in oxidative stress markers (MDA).
Shortened escape latency and increased target quadrant time indicate enhanced learning and memory abilities.
Improved neuronal structure was observed in the hippocampal CA1 region, with ELISA detecting elevated BDNF levels and decreased AChE levels in the hippocampus.
Inhibition of the hippocampal NLRP3 inflammasome pathway (e.g., reduced expression of NLRP3, ASC, caspase-1, GSDMD, and IL-1β).
分子量

168.19

Formula

C9H12O3
CAS 号
性状

液体

中文名称

羟基氢醌三甲醚
运输条件

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

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
纯度 & 产品资料
参考文献

1,2,4-Trimethoxybenzene 相关分类

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Keywords:

1,2,4-Trimethoxybenzene135-77-3羟基氢醌三甲醚NOD-like Receptor (NLR)CaspaseInterleukin RelatedILessential oilsNLRP3 inflammasomeASCexperimental autoimmune encephalomyelitisInhibitorinhibitorinhibit

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