2. Epigenetics PI3K/Akt/mTOR Immunology/Inflammation Metabolic Enzyme/Protease
  3. AMPK Nuclear Factor of activated T Cells (NFAT) Interleukin Related Endogenous Metabolite
  4. NFAT-133

NFAT-133 是一种具有免疫抑制和抗糖尿病活性的芳香族聚酮化合物。NFAT-133 激活 AMPK 通路，促进 L6 肌管的葡萄糖摄取，从而抵抗糖尿病。NFAT-133 通过抑制活化 T 细胞核因子 (NFAT) 的转录活性，进而抑制 IL-2 的表达和 T 细胞增殖，表现出免疫抑制作用。NFAT-133 未表现出抗菌活性或细胞毒性，但能轻微抑制脂多糖 (LPS) (HY-D1056) 诱导的 RAW264.7 细胞中 NO 的产生。

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NFAT-133

NFAT-133 Chemical Structure

CAS No. : 165133-85-7

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NFAT-133 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NFAT-133 is an aromatic polyketide with immunosuppressive and antidiabetic activity. NFAT-133 activates the AMPK pathway, promoting glucose uptake in L6 muscle fibers, thereby resisting diabetes. NFAT-133 inhibits the transcriptional activity of activated T-cell nuclear factor (NFAT), thereby suppressing the expression of IL-2 and the proliferation of T cells, demonstrating an immunosuppressive effect. NFAT-133 does not exhibit antibacterial activity or cytotoxicity, but it can weaken the production of NO in RAW264.7 cells induced by Lipopolysaccharide (LPS) (HY-D1056)[1][2][3][4].

IC50 & Target[1][2]

AMPK

 

IL-2

 

体外研究
(In Vitro)

NFAT-133 (0.01-100 μM，0.5-24 小时) 以剂量和时间依赖性方式刺激葡萄糖摄取，在大鼠 L6 肌管中的 EC₅₀ 值为 1.5 μM，且具有低细胞毒性[2]。
NFAT-133 (3 μM，16 小时) 激活 AMPK-ACC 信号轴，并最终通过磷酸化大鼠 L6 肌管中的 AS160 促进 GLUT4 易位至细胞膜 (其作用机制不依赖于胰岛素信号通路 (PI3K/Akt))[2]。
NFAT-133 (0-50 μM) 对金黄色葡萄球菌 ATCC 12600、枯草芽孢杆菌 ATCC 6051、大肠杆菌 ATCC 11775 和铜绿假单胞菌 ATCC 9721 均无活性，并且对 RAW264.7、HeLa、NCI-H460 和 MCF-7 细胞无任何细胞毒性[3]。
NFAT-133 (25 小时) 以剂量依赖性方式轻微降低 RAW264.7 细胞中 LPS 诱导的一氧化氮 (NO) 的产生[3]。
NFAT-133 (100 μM) 无法激活大鼠 L6 肌管中的 PPARγ，从而避免了体重增加、肝毒性和心血管风险等副作用[4]。

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

NFAT-133 相关抗体:

Western Blot Analysis[2]

Cell Line: Rat L6 myotubes
Concentration: 3 μM
Incubation Time: 16 h
Result: Stimulated AMPK activation but Akt.
Mediated AMPK activation did not affect CAMKKβ and LKB1.
Promoted AS160 phosphorylation and GLUT4 translocation.
药代动力学
(Parmacokinetics)[4]
Species Dose Route Indicator value
Mice 30 mg/kg i.p. Tmax 0.08 h
Mice 30 mg/kg p.o. Tmax 0.08 h
Mice 30 mg/kg i.p. Cmax 11.653 μg/mL
Mice 30 mg/kg p.o. Cmax 3.41 μg/mL
Mice 30 mg/kg i.p. Cmax 42.221 μM
Mice 30 mg/kg p.o. Cmax 12.34 μM
Mice 30 mg/kg i.p. AUClast 3.217
Mice 30 mg/kg p.o. AUClast 0.63
Mice 30 mg/kg i.p. AUC0-inf 3.553
Mice 30 mg/kg p.o. AUC0-inf 0.65
Mice 30 mg/kg i.p. T1/2 1.86 h
Mice 30 mg/kg p.o. T1/2 0.16 h
体内研究
(In Vivo)

NFAT-133 (100 mg/kg，腹腔注射，每天两次，持续 10 天) 显著降低糖尿病小鼠的血糖和胰岛素水平[4]。

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

Animal Model: Diabetes model established in l male db/db mice (7-9 weeks of age)[1]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection (i.p.), twice daily for 10 days
Result: Significantly reduced blood sugar and insulin levels without increasing the weight of the liver or the body weight of the mice.
分子量

276.37

Formula

C17H24O3
CAS 号
结构分类
初始来源

Dactylosporangium
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

NFAT-133 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:

NFAT-133165133-85-7NFAT133NFAT 133AMPKNuclear Factor of activated T Cells (NFAT)Interleukin RelatedEndogenous MetaboliteAMP-activated protein kinaseILGlucose uptakeL6 myotubesMitochondrial membrane potentialAMP/ATP ratioInhibitorinhibitorinhibit

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HY-N16431
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